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Results for "

5-HT2

" in MCE Product Catalog:

By Targets:	5-HT Receptor (233) Adenylate Cyclase (2) Adrenergic Receptor (33) Apoptosis (8) Autophagy (12) Bacterial (3) Calcium Channel (2) Cannabinoid Receptor (1) Chloride Channel (1) Cytochrome P450 (1) Dopamine Receptor (80) Drug Metabolite (2) DYRK (2) Endogenous Metabolite (5) GABA Receptor (1) GlyT (2) Histamine Receptor (12) Influenza Virus (1) Isotope-Labeled Compounds (1) mAChR (5) Melatonin Receptor (8) Mitophagy (2) Monoamine Oxidase (3) Orexin Receptor (OX Receptor) (2) P-glycoprotein (4) P2X Receptor (4) Parasite (1) Phosphatase (1) Potassium Channel (4) Serotonin Transporter (3) Sigma Receptor (5) Sodium Channel (2) TRP Channel (1)
By Research Areas:	Cancer (18) Cardiovascular Disease (16) Endocrinology (22) Infection (5) Inflammation/Immunology (18) Metabolic Disease (14) Neurological Disease (216)

By Targets:

5-HT Receptor (233)

Adenylate Cyclase (2)

Adrenergic Receptor (33)

Apoptosis (8)

Autophagy (12)

Bacterial (3)

Calcium Channel (2)

Cannabinoid Receptor (1)

Chloride Channel (1)

Cytochrome P450 (1)

Dopamine Receptor (80)

Drug Metabolite (2)

DYRK (2)

Endogenous Metabolite (5)

GABA Receptor (1)

GlyT (2)

Histamine Receptor (12)

Influenza Virus (1)

Isotope-Labeled Compounds (1)

mAChR (5)

Melatonin Receptor (8)

Mitophagy (2)

Monoamine Oxidase (3)

Orexin Receptor (OX Receptor) (2)

P-glycoprotein (4)

P2X Receptor (4)

Parasite (1)

Phosphatase (1)

Potassium Channel (4)

Serotonin Transporter (3)

Sigma Receptor (5)

Sodium Channel (2)

TRP Channel (1)

By Research Areas:

Cancer (18)

Cardiovascular Disease (16)

Endocrinology (22)

Infection (5)

Inflammation/Immunology (18)

Metabolic Disease (14)

Neurological Disease (216)

254

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas

HY-U00365

5-HT2 antagonist 1	5-HT Receptor Adrenergic Receptor	Cardiovascular Disease Endocrinology
5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.

HY-145841

5-HT2A receptor agonist-2	5-HT Receptor	Cardiovascular Disease
5-HT2A receptor agonist-2 is a highly potent serotonin 5-HT2 receptor agonists. 5-HT2A receptor agonist-2 inspires 5-HT_2A, 5-HT_2B, and 5-HT_2C with EC₅₀ values of 1.7, 0.58, and 0.50 nM, respectively.

HY-147203

5-HT2B antagonist-1	5-HT Receptor	Cancer Endocrinology Metabolic Disease Cardiovascular Disease
5-HT2B antagonist-1 is an orally active *5-HT2B* receptor antagonist with an IC₅₀ value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease.

HY-U00286

5-HT2A antagonist 1	5-HT Receptor	Cardiovascular Disease
5-HT2A antagonist 1 is a *5-HT2A* antagonist extracted from patent US5728835A and JP 1007727. 5-HT2A antagonist 1 may be useful in treatment of gastrointestinal disorders circulatory disorders.

HY-100971

Spiramide AMI-193	5-HT Receptor Dopamine Receptor	Neurological Disease
Spiramide (AMI-193) is a potent and selective antagonist of *5-HT₂* and dopamine D2 receptor, with K_is of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT₂ versus 5-HT_1C (K_i=4300 nM) receptors. Spiramide exhibits antipsychotic activity.

HY-103104

Fananserin RP 62203	5-HT Receptor Dopamine Receptor	Neurological Disease
Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT₂) receptor antagonist, with a K_i of 0.37 nM for the rat 5-HT_2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a K_i of 2.93 nM for the human dopamine D4 receptor.

HY-103148

LY215840
5-HT Receptor Neurological Disease

LY215840, a 5-HT₇ receptor ligand and a 5-HT₂ receptor antagonist, blocks serotonin-induced relaxation in canine coronary artery.

LY215840	5-HT Receptor	Neurological Disease
LY215840, a 5-HT₇ receptor ligand and a 5-HT₂ receptor antagonist, blocks serotonin-induced relaxation in canine coronary artery.

HY-136281

DuP 734	Sigma Receptor	Neurological Disease
DuP 734 is a sigma receptor antagonist. DuP 734 is a selective and potent sigma and 5-HT2 receptor ligand with weak affinity for D2 receptors. DuP 734 may have antipsychotic activity without the liability of motor side effects typical of neuroleptics.

HY-W011040

LY320135	Cannabinoid Receptor 5-HT Receptor mAChR	Neurological Disease
LY320135 is a potent and selective antagonist of CB1 receptor, with a K_i of 141 nM. LY320135 also binds to *5-HT₂* and muscarinic receptors with K_is of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.

HY-100943

Cinanserin hydrochloride SQ 10643	5-HT Receptor Influenza Virus	Infection Inflammation/Immunology
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT₂ receptor antagonist with a K_i of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the *5-HT₂* than for the 5-HT₁ receptor (K_i of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.

HY-10563

Sarpogrelate MCI-9042 free acid	5-HT Receptor	Infection
Sarpogrelate (MCI-9042) is a new, specific orally active *5-HT₂* receptor antagonist, Sarpogrelate increases platelet aggregation and has hemostasis effect, and can be used for the research of Buerger’s disease.

HY-B0352A

(S)-Mirtazapine (S)-Org3770; (S)-6-Azamianserin	5-HT Receptor	Neurological Disease
(S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception. (S)-Mirtazapine is a stereoselective 5-HT₂ receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.

HY-14325A

L-745870 trihydrochloride	Dopamine Receptor	Neurological Disease
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

HY-151596

*MAO-A/5-HT2AR-IN-1*	Monoamine Oxidase 5-HT Receptor	Neurological Disease
MAO-A/5-HT2AR-IN-1 (compound I14) is a potent MAO-A and *5-HT2AR* dual inhibitor, with IC₅₀ values of 0.004 and 0.014 μM, respectively. MAO-A/5-HT2AR-IN-1 is a potential antidepressant agent.

HY-101632

Irindalone
Lu 21-098
5-HT Receptor Neurological Disease

Irindalone is a novel serotonin 5-HT₂ antagonist.

Irindalone Lu 21-098	5-HT Receptor	Neurological Disease
Irindalone is a novel serotonin *5-HT₂* antagonist.

HY-B0352

Mirtazapine Org3770; 6-Azamianserin	5-HT Receptor Histamine Receptor Adrenergic Receptor	Inflammation/Immunology Neurological Disease Cancer
Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a *5-HT₂, 5-HT₃, histamine H1 receptor* and α2-adrenoceptor antagonist with pK_i values of 8.05, 8.1, 9.3 and 6.95, respectively.

HY-14940

Volinanserin MDL100907; M 100907	5-HT Receptor	Neurological Disease
Volinanserin is a potent and selective antagonist of 5-HT₂ receptor, with a K_i of 0.36 nM, and shows 300-fold selectivity for 5-HT₂ receptor over 5-HT_1c, alpha-1 and DA D₂ receptors. Volinanserin has antipsychotic activity.

HY-145862

5-HT6/5-HT2AR antagonist-1
5-HT Receptor Neurological Disease

5-HT6/5-HT2AR antagonist-1 is a potent dual 5-HT₆/5-HT_2AR antagonist with K_i values of 11 nM and 39 nM, respectively.
HY-B1737

Pirenperone
R 47465
5-HT Receptor Neurological Disease

Pirenperone (R 47465) is a 5-HT₂ serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity.

*5-HT6/5-HT2AR antagonist-1*	5-HT Receptor	Neurological Disease
5-HT6/5-HT2AR antagonist-1 is a potent dual *5-HT₆/5-HT_2AR* antagonist with K_i values of 11 nM and 39 nM, respectively.

Pirenperone R 47465	5-HT Receptor	Neurological Disease
Pirenperone (R 47465) is a 5-HT₂ serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity.

HY-146077

*5-HT6/5-HT2A receptor ligand-2*	5-HT Receptor	Neurological Disease
5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT₆/5-HT_2A receptor antagonist, with a K_i of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties.

HY-146076

*5-HT6/5-HT2A receptor ligand-1*	5-HT Receptor	Neurological Disease
5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT₆/5-HT_2A receptor antagonist, with a K_i of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research.

HY-14940S

Volinanserin-d4 hydrochloride	5-HT Receptor	Neurological Disease
Volinanserin-d₄ (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1][2].

HY-B0115

Pizotifen
Pizotyline; BC-105
5-HT Receptor Neurological Disease

Pizotifen (Pizotyline) is a potent 5-HT₂ receptor antagonist, with a high affinity for 5-HT_1C binding site.

Pizotifen Pizotyline; BC-105	5-HT Receptor	Neurological Disease
Pizotifen (Pizotyline) is a potent *5-HT₂* receptor antagonist, with a high affinity for 5-HT_1C binding site.

HY-11018

Risperidone R 64 766	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-11018A

Risperidone hydrochloride R 64 766 hydrochloride	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone hydrochloride (R 64 766 hydrochloride) 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-B0115A

Pizotifen malate Pizotyline malate; BC-105 malate	5-HT Receptor	Neurological Disease
Pizotifen malate (Pizotyline malate) is a potent *5-HT₂* receptor antagonist, with a high affinity for 5-HT_1C binding site.

HY-11018B

Risperidone mesylate R 64 766 mesylate	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone mesylate(R 64 766 mesylate) is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-10562

Ketanserin R41468	5-HT Receptor Potassium Channel Autophagy	Neurological Disease
Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (I_hERG) in a concentration-dependent manner (IC₅₀=0.11 μM).

HY-113643

Levemopamil hydrochloride	Calcium Channel 5-HT Receptor	Neurological Disease
Levemopamil hydrochloride is a blood-brain barrier penetrable calcium channel blocker and a *5-HT2* antagonist. Levemopamil hydrochloride can be used for temporary occlusion and neurological disease research.

HY-N4157

Isopteropodine	mAChR 5-HT Receptor	Neurological Disease
Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and *5-HT2* receptors.

HY-B1107

Naftidrofuryl oxalate Nafronyl oxalate salt	5-HT Receptor	Cardiovascular Disease
Naftidrofuryl oxalate (Nafronyl oxalate salt) is a drug used in the management of peripheral and cerebral vascular disorders as a vasodilator, enhance cellular oxidative capacity, and may also be a 5-HT2 receptor antagonist.

HY-110232

Risperidone-d4 R 64 766-d₄	5-HT Receptor Dopamine Receptor P-glycoprotein	Neurological Disease
Risperidone-d₄ is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.

HY-135194

Risperidone E-oxime	Drug Metabolite	Others
Risperidone E-oxime is an impurity of Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .

HY-U00367

(4E)-SUN9221	Adrenergic Receptor 5-HT Receptor	Cardiovascular Disease Endocrinology
(4E)-SUN9221 is a potent antagonist of α1-adrenergic receptor and 5-HT2 receptor, with antihypertensive and anti-platelet aggregation activities.

HY-101094

Ocaperidone R79598	5-HT Receptor Dopamine Receptor	Neurological Disease
Ocaperidone is an effective antipsychotic agent, acting as a potent *5-HT₂* and dopamine D₂ antagonist, and a 5-HT_1A agonist, with K_is of 0.14 nM, 0.46 nM, 0.75 nM, 1.6 nM and 5.4 nM for 5-HT₂, a₁-adrenergic receptor, dopamine D₂, histamine H₁ and a₂-adrenergic receptor, respectively, and a pEC₅₀ and pK_i of 7.60 and 8.08 for h5-HT_1A.

HY-10562A

Ketanserin tartrate R41468 tartrate	5-HT Receptor Potassium Channel Autophagy	Neurological Disease
Ketanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (I_hERG) in a concentration-dependent manner (IC₅₀=0.11 μM).

HY-119156

Altanserin
5-HT Receptor Others

Altanserin can synthesize Fluorine-18 Altanserin. Fluorine-18 Altanserin binds to the brain 5HT₂ receptors.

Altanserin	5-HT Receptor	Others
Altanserin can synthesize Fluorine-18 Altanserin. Fluorine-18 Altanserin binds to the brain 5HT₂ receptors.

HY-B0352S

Mirtazapine D3 Org3770 d₃; 6-Azamianserin d₃	5-HT Receptor	Neurological Disease
Mirtazapine-d₃ is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors[1].

HY-10791

Ritanserin R 55667	5-HT Receptor Histamine Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT₂ receptor, with an IC₅₀ of 0.9 nM, less active on Histamine H₁, Dopamine D₂, Adrenergic α₁, Adrenergic α₂ receptors.

HY-B1213S

Trimipramine-d3 maleate	5-HT Receptor Bacterial	Neurological Disease
Trimipramine-d₃ (maleate) is the deuterium labeled Trimipramine maleate. Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively[1][2].

HY-B0352AS

(S)-Mirtazapine-d3 (S)-Org3770 d₃; (S)-6-Azamianserin d₃	5-HT Receptor	Neurological Disease
(S)-Mirtazapine-d₃ is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].

HY-14325

L-745870	Dopamine Receptor	Neurological Disease
L-745870 is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

HY-14325B

L-745870 hydrochloride	Dopamine Receptor	Neurological Disease
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D₄ receptor antagonist with a K_i of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D₂ (K_i of 960 nM) and D₃ (K_i of 2300 nM) receptors, and exhibits moderate affinity for 5-HT₂ receptors, sigma sites and α-adrenoceptors.

HY-B1213A

Trimipramine	5-HT Receptor Bacterial	Neurological Disease
Trimipramine is a 5-HT receptor antagonist, with pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC₅₀ values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy.

HY-B1213

Trimipramine maleate	5-HT Receptor Bacterial	Neurological Disease
Trimipramine maleate is a 5-HT receptor antagonist, with pK_i binding values of 6.39, 8.10, 4.66 for 5-HT_1C, 5-HT₂ and 5-HT_1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC₅₀ values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy.

HY-101009

Methiothepin maleate Metitepine maleate; Ro-8-6837 maleate	5-HT Receptor	Neurological Disease
Methiothepin maleate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

HY-19358

2-Methyl-5-HT 2-Methyl-5-hydroxytryptamine; 2-Methylserotonin; 2-Me-5-HT	5-HT Receptor	Neurological Disease
2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT₃ receptor agonist. 2-Methyl-5-HT is shown to display anti-depressive-like effects.

HY-107836

Methiothepin mesylate Metitepine mesylate; Ro 8-6837 mesylate	5-HT Receptor	Neurological Disease
Methiothepin (Metitepine) mesylate is a potent and non-selective 5-HT₂ receptor antagonist, with pK_ds of 7.10 (5-HT_1A), 7.28 (5HT_1B), 7.56 (5HT_1C), 6.99 (5HT_1D), 7.0 (5-HT_5A), 7.8 (5-HT_5B), 8.74 (5-HT₆), and 8.99 (5-HT₇), and pK_is of 8.50 (5HT_2A), 8.68 (5HT_2B), and 8.35 (5HT_2C).

HY-19686

Ipsapirone TVX Q 7821 free base	5-HT Receptor	Neurological Disease
Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT_1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT_1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT₂ and the α₁-adrenergic function.

HY-108400

SCH-23390 maleate R-(+)-SCH-23390 maleate	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 maleate is a potent and high efficacy *human 5-HT_2C* receptor agonist with a K_i of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀** of 268 nM.

HY-19545A

SCH-23390 hydrochloride R-(+)-SCH-23390 hydrochloride	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy *human 5-HT_2C* receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT₂ and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀** of 268 nM.

HY-B0352S2

Mirtazapine-d4 Org3770-d₄; 6-Azamianserin-d₄	5-HT Receptor Histamine Receptor Adrenergic Receptor	Inflammation/Immunology Neurological Disease
Mirtazapine-d₄ is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].

HY-12697

NGB 2904	Dopamine Receptor	Neurological Disease
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a K_i of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis.

HY-12697A

NGB 2904 hydrochloride	Dopamine Receptor	Neurological Disease
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a K_i of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (K_is=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis.

HY-103151

CP94253 hydrochloride	5-HT Receptor	Neurological Disease
CP94253 hydrochloride is a potent and selective agonist of 5-HT_1B receptor (K_i= 2 nM in a radioligand binding assay).K_i values for 5-HT_1A, 5-HT_1D, 5-HT_1C and 5-HT₂ receptors are 89, 49, 860, and 1600 nM respectively. CP94253 hydrochloride is centrally active upon systemic administration in vivo.

HY-103413

Eticlopride hydrochloride	Dopamine Receptor	Neurological Disease
Eticlopride hydrochloride, a selective dopamine D2‐like receptor antagonist, exhibits high affinity for dopamine D2, α1‐adrenergic, α2‐adrenergic, 5HT1, 5HT2 receptors with K_is of 0.09, 112, 699, 6220, and 830 nM, respectively. Antipsychotic agent.

HY-14541

Olanzapine LY170053	5-HT Receptor Dopamine Receptor mAChR Adrenergic Receptor Autophagy Mitophagy Apoptosis	Neurological Disease Cancer
Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to *serotonin H1, 5HT2A/2C, 5HT3, 5HT6* (K_i=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (K_i=11 to 31 nM), muscarinic M1-5 (K_i=1.9-25 nM), and adrenergic α1 receptor (K_i=19 nM). Olanzapine is an atypical antipsychotic.

HY-103094

LY266097 hydrochloride	5-HT Receptor	Inflammation/Immunology
LY266097 hydrochloride is a selective *5-HT2B* receptor antagonist with pK_is of 7.7, 9.8, and 7.6 for *5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2*B receptor blockade contributes to the research in depression.

HY-103120

Org37684	5-HT Receptor	Neurological Disease
Org37684 is a highly potent 5-HT_2C receptor agonist (pEC₅₀=8.17). Org37684 exhibits a rank order of potency of 5-HT_2C>5-HT_2B>5-HT_2A. Its selectivity for the 5-HT2C receptor is approximately 2.5 times over the 5-HT2B (pEC₅₀=7.96) and ten times for the 5-HT_2A (pEC₅₀=7.11) receptor.

HY-101250

Glemanserin MDL11939	Serotonin Transporter	Neurological Disease
Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor *5-HT_2A* (K_i=2.89, 0.54 and 2.5 nM for rat 5-HT_2A, rabbit 5-HT_2A and human 5-HT_2A, respectively).

HY-103129A

SB-200646	5-HT Receptor	Neurological Disease
SB-200646 is the first selective *5-HT_2B/2C* over 5-HT_2A receptor antagonist with pK_i values of 7.5, 6.9 and 5.2 for *5-HT_2B, 5-HT_2C* and 5-HT_2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo.

HY-103129

SB-200646A	5-HT Receptor	Neurological Disease
SB-200646A is the first selective *5-HT_2B/2C* over 5-HT_2A receptor antagonist with pK_i values of 7.5, 6.9 and 5.2 for *5-HT_2B, 5-HT_2C* and 5-HT_2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.

HY-103135

SB 206553 hydrochloride	5-HT Receptor	Neurological Disease
SB 206553 hydrochloride is a high affinity, selective and orally active 5-HT_2B / 5-HT_2C receptor antagonist (rat 5-HT_2B pA2 = 8.89, human 5-HT_2C pKi = 7.92). SB 206553 possesses anxiolytic-like properties.

HY-18596

SB-215505	5-HT Receptor	Neurological Disease
SB-215505 is a potent and subtype-selective *5-HT_2B* receptor antagonist with pK_i values of 8.3, 6.77, 7.66 for 5-HT_2B, 5-HT_2A, 5-HT_2C, respectively. SB-215505 increases wakefulness and motor activity in rats.

HY-103155

SB-221284	5-HT Receptor	Neurological Disease
SB 221284 is a selective *5-HT_2C/2B* receptor antagonist with pK_i values are 6.4, 7.9 and 8.6 for *5-HT_2A, 5-HT_2B* and *5-HT_2C* receptors, respectively. SB 221284 can be used for the research of neurological disease.

HY-10792

Eplivanserin SR-46349	5-HT Receptor	Neurological Disease
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT_2A receptor antagonist, with an IC₅₀ of 5.8 nM in rat cortical membrane, and a K_d of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for *5-HT_2A* than 5-HT_2B and 5-HT_2C.

HY-110129

Eplivanserin hemifumarate SR-46349 hemifumarate; SR 46349B	5-HT Receptor	Neurological Disease
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT_2A receptor antagonist, with an IC₅₀ of 5.8 nM in rat cortical membrane, and a K_d of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for *5-HT_2A* than 5-HT_2B and 5-HT_2C.

HY-103154

SB228357	5-HT Receptor	Neurological Disease
SB228357 is a selective, potent and orall active 5-HT_2C/2B receptor antagonist with pK_i values of 6.9, 8.0 and 9.0 for *5-HT_2A, 5-HT_2B* and *5-HT_2C*, respectively. SB228357 has antidepressant/anxiolytic effects.

HY-21994

Org-12962 hydrochloride	5-HT Receptor	Neurological Disease
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT_2C receptor agonist and exhibits pEC₅₀ values of 7.01, 6.38 and 6.28 for 5-HT_2C, 5-HT_2A and 5-HT_2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.

HY-101630

Deramciclane EGIS-3886	5-HT Receptor	Neurological Disease
Deramciclane has a high affinity for *5-HT_2A* and *5-HT_2C* receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT_2C receptors without direct stimulatory agonist.

HY-103144

WAY 629 hydrochloride	5-HT Receptor	Neurological Disease
WAY 629 hydrochloride is a potent and selective *5-HT_2C* agonist with EC₅₀s of 426, 260000 nM for 5-HT_2C and 5-HT_2A, respectively. WAY 629 hydrochloride decreases feeding behavior.

HY-W380450

Viloxazine Viloxazin; Emovit	5-HT Receptor Adrenergic Receptor	Neurological Disease
Viloxazine (Viloxazin) is a norepinephrine reuptake inhibitor, also a potent *5-HT_2C* agonist and *5-HT_2B* antagonist with an EC₅₀ of 32 μM and an IC₅₀ of 27 μM for 5-HT_2C and 5-HT_2B, respectively. The mechanism of action of Viloxazine predominantly involves serotonergic and noradrenergic pathways. Viloxazine can be used for researching depression.

HY-103138

(Rac)-WAY-161503 hydrochloride	5-HT Receptor	Metabolic Disease Neurological Disease
(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity 5-HT_2C receptor agonist with a K_i of 4 nM and an EC₅₀ of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT_2C than 5-HT_2A and 5-HT_2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects.

HY-103138A

(Rac)-WAY-161503	5-HT Receptor	Metabolic Disease Neurological Disease
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT_2C receptor agonist with a K_i of 4 nM and an EC₅₀ of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT_2C than 5-HT_2A and 5-HT_2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects.

HY-10559

Nelotanserin APD125	5-HT Receptor	Cancer Neurological Disease
Nelotanserin is a potent *5-HT_2A* inverse agonist, a moderately potent *5-HT_2C* partial inverse agonist and a weak *5-HT_2B* inverse agonist, with IC₅₀s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

HY-101365

RS-102221	5-HT Receptor	Neurological Disease
RS-102221 is a selective 5-HT2C receptor antagonist (K_i=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the *5-HT2A* and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats.

HY-101365A

RS-102221 hydrochloride	5-HT Receptor	Neurological Disease
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (K_i=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the *5-HT2A* and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats.

HY-117118A

AC-90179
5-HT Receptor Neurological Disease

AC-90179 is a selective 5-HT2A receptor inverse agonist (K_i = 2.1 nM) and 5-HT2C antagonist, a potential antipsychotic compound.
HY-100330

YM348
5-HT Receptor Metabolic Disease

YM348 is a potent and orally active 5-HT_2C receptor agonist, which shows a high affinity for cloned human 5-HT_2C receptor (K_i: 0.89 nM).

HY-133024

Flumexadol	5-HT Receptor	Neurological Disease
Flumexadol is a selective and affinity 5-HT_2C receptor agonist with a K_i of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT_2A receptor. Flumexadol is an orally active non-narcotic analgesic.

HY-100970

4F 4PP oxalate	5-HT Receptor	Neurological Disease
4F 4PP (oxalate) is a selective *5-HT2A* antagonist with almost as high affinity (K_i= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (K_i= 620 nM).

HY-10564

Sarpogrelate hydrochloride MCI-9042	5-HT Receptor	Cardiovascular Disease
Sarpogrelate hydrochloride (MCI-9042) is a selective *5-HT₂R* antagonist, with pK_is of 8.52, 6.57, and 7.43 for 5-HT_2A, 5-HT_2B, and 5-HT_2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT₁, 5-HT₃, 5-HT₄, α₁-, α₂- and β-adrenoreceptor, histamine H₁, H₂ and muscarinic M₃ receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.

HY-14153

Tegaserod	5-HT Receptor Apoptosis	Cancer Metabolic Disease
Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a *5-HT_2B* receptor antagonist. Tegaserod has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.

HY-B0781

Promethazine hydrochloride	Histamine Receptor	Neurological Disease Endocrinology
Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

HY-14546

Aripiprazole OPC-14597	5-HT Receptor Dopamine Receptor	Infection Inflammation/Immunology Neurological Disease
Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at *5-HT2B* and *5-HT2A* receptors and displays partial agonist actions at 5-HT1A, *5-HT2C*, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.

HY-14546A

Aripiprazole monohydrate OPC-14597 monohydrate	5-HT Receptor Dopamine Receptor	Infection Inflammation/Immunology Neurological Disease
Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at *5-HT2B* and *5-HT2A* receptors and displays partial agonist actions at 5-HT1A, *5-HT2C*, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19.

HY-10560

Temanogrel
APD791
5-HT Receptor Neurological Disease

Temanogrel is a highly selective 5-HT_2A receptor antagonist with a K_i of 4.9 nM.

HY-113008A

cis-Urocanic acid (Z)-Urocanic acid; cis-UCA	5-HT Receptor	Inflammation/Immunology
cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (K_d=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.

HY-19469

Roluperidone CYR-101; MIN-101; MT-210	5-HT Receptor Sigma Receptor	Neurological Disease
Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for *5-HT_2A* and sigma-2 receptors (K_i of 7.53 nM and 8.19 nM for 5-HT_2A and sigma-2, respectively).

HY-14264

Cyamemazine	5-HT Receptor	Neurological Disease
Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT₃ (K_i of 12 nM), *5-HT_2A* (K_i = 1.5 nM) and *5-HT_2C* (K_i of 75 nM) receptors antagonist with antipsychotic activity.

HY-14543

Sertindole Lu 23-174	5-HT Receptor Dopamine Receptor Adrenergic Receptor Autophagy	Neurological Disease Cancer
Sertindole (Lu 23-174) is an orally active *5-HT_2A, 5-HT_2C, dopamine D₂, and αl-adrenergic* receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells.

HY-118152

Org-12962	5-HT Receptor	Neurological Disease
Org-12962 is a potent, selective and orally active *5-HT_2C receptor* agonist with a pEC₅₀ value of 7.01. Org-12962 also exhibits high effacy for the 5-HT_2A and 5-HT_2B receptor with pEC₅₀s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.

HY-B1033

Metergoline	5-HT Receptor Dopamine Receptor Sodium Channel	Neurological Disease
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pK_is of 8.64, 8.75 and 8.75 for 5-HT_2A, 5-HT_2B and 5-HT_2C, respectively. Metergoline is a high-affinity ligand for the h5-HT₇ receptor, with a K_i of 16 nM. Metergoline is also a reversible neural Na⁺ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.

HY-14153A

Tegaserod maleate SDZ-HTF-919; HTF-919	5-HT Receptor Apoptosis	Metabolic Disease Neurological Disease
Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT₄R) agonist and a *5-HT_2B* receptor antagonist. Tegaserod maleate has pK_is of 7.5, 8.4 and 7.0 for human recombinant 5-HT_2A, 5-HT_2B and 5-HT_2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.

HY-10564S

Sarpogrelate-d3 hydrochloride MCI-9042-d₃	5-HT Receptor	Cardiovascular Disease
Sarpogrelate-d₃ (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].

HY-101755

Tedatioxetine hydrobromide Lu AA24530 hydrobromide	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and *5-HT_2A, 5-HT_2C, 5-HT₃* and α_1A-adrenergic receptor antagonist . ,

HY-N0145

Puerarin
5-HT Receptor Inflammation/Immunology Cancer

Puerarin, an isoflavone extracted from Radix puerariae, is a 5-HT2C receptor antagonist.

HY-19417A

Wf-516	Serotonin Transporter 5-HT Receptor	Neurological Disease
Wf-516 is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and *5-HT2A* receptors, with K_i of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.

HY-B0781S

Promethazine-d4 hydrochloride	Histamine Receptor	Neurological Disease Endocrinology
Promethazine-d₄ (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

HY-B1101

Pimethixene Pimetixene	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.

HY-B1101A

Pimethixene maleate Pimetixene maleate	5-HT Receptor Histamine Receptor	Neurological Disease Endocrinology
Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, histamine H₁, dopamine D₂ and D_4.4 as well as muscarinic M₁ and M₂ receptors, with pK_is of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.

HY-15401

WAY 163909
5-HT Receptor Cancer

WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a K_i of 10.5±1.1 nM.
HY-103140

Ro60-0175 fumarate
5-HT Receptor Neurological Disease

Ro60-0175 fumarate is a potent and selective agonist of 5-HT_2C receptor.
HY-103153

SB 204741
5-HT Receptor Cardiovascular Disease

SB 204741 is a selective and high affinity 5-HT_2B antagonist with a pK_i value of 7.1.

HY-14264S

Cyamemazine-d6	5-HT Receptor	Neurological Disease
Cyamemazine-d₆ is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity[1][2].

HY-100171

PRX933 hydrochloride GW876167 hydrochloride; BVT-933 hydrochloride	5-HT Receptor	Cardiovascular Disease
PRX933 hydrochloride is a 5-HT_2c receptor agonist extracted from patent WO 2014140631 A1.

HY-111200

Vabicaserin hydrochloride
SCA 136
5-HT Receptor Neurological Disease

Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT_2C) receptor-selective agonist with an EC₅₀ of 8 nM.

HY-113008AS

cis-Urocanic acid-13C3 (Z)-Urocanic acid-¹³C₃; cis-UCA-¹³C₃	5-HT Receptor	Inflammation/Immunology
cis-Urocanic acid-¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].

HY-14557

Pimavanserin
ACP-103
5-HT Receptor Neurological Disease

Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-103093

Zotepine	5-HT Receptor Histamine Receptor Adrenergic Receptor Dopamine Receptor	Neurological Disease
Zotepine, an antipsychotic agent, is a potent antagonist of *5-HT_2A, 5-HT_2C, Histamine H₁, α₁-adrenergic* and Dopamine D₂ receptors, with K_ds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo.

HY-101619

Abaperidone
Dopamine Receptor 5-HT Receptor Neurological Disease

Abaperidone is a potent antagonist of 5-HT_2A receptor and dopamine D₂ receptor with IC₅₀s of 6.2 and 17 nM.
HY-101815

Lidanserin
ZK-33839
5-HT Receptor Adrenergic Receptor Neurological Disease Endocrinology

Lidanserin (ZK-33839) acts as a 5-HT_2A and α₁-adrenergic receptor antagonist.

HY-N0049

Nuciferine	5-HT Receptor Dopamine Receptor	Neurological Disease
Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), *5-HT_2C* (IC₅₀=131 nM), and *5-HT_2B* (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-141422A

4,4-Diphenylbutylamine hydrochloride	5-HT Receptor	Neurological Disease
4,4-Diphenylbutylamine shows affinity for the *5-HT_2A* and H₁ receptors with K_is of 2589 and 1670 nM, respectively.

HY-15543A

CP-809101 hydrochloride	5-HT Receptor	Neurological Disease
CP-809101 hydrochloride is a potent and highly selective *5-HT_2C* receptor agonist, with pEC₅₀s of 9.96, 7.19 and 6.81 M for human *5HT_2C, 5HT_2B* and *5HT_2A* receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.

HY-15543

CP-809101	5-HT Receptor	Neurological Disease
CP-809101 is a potent and highly selective *5-HT_2C* receptor agonist, with pEC₅₀s of 9.96, 7.19 and 6.81 M for human *5HT_2C, 5HT_2B* and *5HT_2A* receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.

HY-149247

Antipsychotic agent-2	5-HT Receptor Dopamine Receptor	Neurological Disease
Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT_1A, *5-HT_2A, 5-HT_2C, D₂ and H₁ receptors with K_i*s of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability.

HY-103152

GR 113808	5-HT Receptor	Inflammation/Immunology Neurological Disease
GR 113808 is a potent and highly selective 5-HT₄ receptor antagonist (pK_b= 8.8). GR 113808 shows 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C and 5-HT₃ receptors.

HY-N0775

Isocorynoxeine 7-Isocorynoxeine	5-HT Receptor	Neurological Disease
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of *5-HT_2A* receptor-mediated current response with an IC₅₀ of 72.4 μM.

HY-103112A

SB 243213 dihydrochloride	5-HT Receptor	Neurological Disease
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

HY-103112B

SB 243213	5-HT Receptor	Neurological Disease
SB 243213 is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

HY-32329

Setiptiline Org-8282	5-HT Receptor Adrenergic Receptor	Neurological Disease
Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.

HY-10457

Velusetrag TD-5108	5-HT Receptor	Metabolic Disease Neurological Disease
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT₄ receptor (5-HT4R), with a pK_i of 7.7. Velusetrag exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease.

HY-103112

SB 243213 hydrochloride	5-HT Receptor	Neurological Disease
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

HY-10457A

Velusetrag hydrochloride TD-5108 hydrochloride	5-HT Receptor	Metabolic Disease Neurological Disease
Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT₄ receptor (5-HT₄R), with a pK_i of 7.7. Velusetrag hydrochloride exhibits no affinity (K_i>10 μM) for 5-HT_2A and 5-HT_2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease.

HY-16729A

Relenopride hydrochloride YKP10811 hydrochloride	5-HT Receptor	Inflammation/Immunology
Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT₄ receptor agonist (K_i=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT_2A (K_i=600 nM) and 5-HT_2B receptors (K_i=31 nM) than for 5-HT₄. Relenopride hydrochloride increases gastrointestinal (GI) motility.

HY-123838

Ro60-0175
5-HT Receptor Neurological Disease

Ro60-0175 is a potent and selective agonist of 5-HT_2C receptor. Ro60-0175 reduces self-administration.

HY-N0737

Harmine hydrochloride Telepathine hydrochloride	DYRK 5-HT Receptor	Cancer Neurological Disease
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM.

HY-101690

QF0301B	Adrenergic Receptor	Cardiovascular Disease Endocrinology
QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.

HY-135392

N-Desmethyl Pimavanserin AC-279	Drug Metabolite	Neurological Disease
N-Desmethyl Pimavanserin is the active metabolite of Pimavanserin. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC₅₀ and pK_d of 8.73 and 9.3, respectively.

HY-106136

TIK-301 PD-6735; LY-156735	Melatonin Receptor 5-HT Receptor	Neurological Disease
TIK-301 (PD-6735) is a chlorinated melatonin derivative and a potent, high-affinity and orally active melatonin MT₁ and MT₂ receptors agonist with K_is of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT_2B/5-HT_2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment.

HY-15472

PRX-08066	5-HT Receptor	Cardiovascular Disease
PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.

HY-133113

7-Desmethyl-agomelatine	5-HT Receptor	Neurological Disease
7-Desmethyl-agomelatine is a metabolite of Agomelatine. Agomelatineis a potent agonist at melatonin receptors (MT1 and MT2), and also is an antagonist of 5-HT2C.

HY-10895

SB-334867 SB 334867A	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

HY-17038A

Agomelatine hydrochloride S-20098 hydrochloride	Melatonin Receptor 5-HT Receptor Endogenous Metabolite	Neurological Disease
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

HY-14544

Quetiapine ICI204636	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, *5-HT2A, 5-HT2C receptor with pK_i*s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.

HY-17038

Agomelatine S-20098	Melatonin Receptor 5-HT Receptor Endogenous Metabolite	Neurological Disease
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

HY-B0031

Quetiapine hemifumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, *5-HT2A, 5-HT2C receptor with pK_i*s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.

HY-32329A

Setiptiline maleate MO-8282	5-HT Receptor	Neurological Disease
Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT_2A, 5-HT_2C, and/or 5-HT₃ subtypes, as well as an H1 receptor inverse agonist/antihistamine.

HY-19283

DU125530	5-HT Receptor	Neurological Disease
DU125530 is a potent and selective5-HT1A receptor antagonist with K_i values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects.

HY-10792A

Eplivanserin (mixture) SR-46349 (mixture)	Serotonin Transporter 5-HT Receptor	Neurological Disease
Eplivanserin mixture (SR-46349 mixture) is a selective serotonin reuptake inhibitor and a 5-HT_2A receptor antagonist, extracted from patent WO 2005/002578 A1.

HY-118557

Iferanserin S-MPEC	5-HT Receptor	Inflammation/Immunology
Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for 5-HT_2A receptor. Iferanserin has the potential for internal hemorrhoid disease treatment.

HY-133111

3-Hydroxy agomelatine	5-HT Receptor	Neurological Disease
3-Hydroxy agomelatine is a metabolite of Agomelatine. 3-Hydroxy agomelatine is a 5-HT_2C receptor antagonist with an IC₅₀ of 3.2 μM and a K_i of 1.8 μM.

HY-B0366A

Cyproheptadine hydrochloride	5-HT Receptor	Neurological Disease Cardiovascular Disease
Cyproheptadine hydrochloride is a potent and orally active 5-HT_2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders.

HY-B1622

Cyproheptadine	5-HT Receptor Apoptosis	Neurological Disease Cardiovascular Disease
Cyproheptadine is a potent and orally active 5-HT_2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders.

HY-118339

PF-4479745	5-HT Receptor	Cancer
PF-4479745 is a potent and selective *5-HT_2C* receptor agonist (EC₅₀: 10 nM, k_i: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension.

HY-13409

SB 242084	5-HT Receptor	Metabolic Disease Neurological Disease
SB 242084 is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT_2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.

HY-13409A

SB 242084 dihydrochloride	5-HT Receptor	Metabolic Disease Neurological Disease
SB 242084 dihydrochloride is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT_2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.

HY-10895A

SB-334867 free base SB334867A free base	Orexin Receptor (OX Receptor)	Neurological Disease Endocrinology
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pK_b=7.4), 100-fold over 5-HT_2B, 5-HT_2C with pK_i values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.

HY-32329S

Setiptiline-d3	5-HT Receptor Adrenergic Receptor	Neurological Disease
Setiptiline-d₃ is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].

HY-N0737A

Harmine Telepathine	DYRK 5-HT Receptor	Cancer Neurological Disease
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM.

HY-16687A

Eltoprazine hydrochloride DU 28853 hydrochloride	5-HT Receptor	Neurological Disease
Eltoprazine hydrochloride (DU 28853 hydrochloride) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.

HY-101324

MK-212
CPP
5-HT Receptor Neurological Disease

MK-212 (CPP) is a centrally acting 5-HT_1C/5-HT₂ agonist. MK-212 can stimulate phosphoinositide hydrolysis in cerebral cortex.

HY-126057S

(R)-Praziquantel-d11	Parasite 5-HT Receptor	Infection
(R)-Praziquantel-d₁₁ is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer[1].

HY-B0031S2

Quetiapine-d8 fumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine-d₈ (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1][2].

HY-100794

GR127935 hydrochloride	5-HT Receptor	Neurological Disease
GR127935 hydrochloride is a potent and orally active 5-HT1D and 5-HT1B receptor antagonist with pKis of 8.5 for both isoforms. GR127935 hydrochloride has 100-fold selectivity for 5-HT1B/1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 hydrochloride can be used in neurological disease research.

HY-17038S1

Agomelatine-d4 S-20098-d₄	Melatonin Receptor 5-HT Receptor Endogenous Metabolite	Neurological Disease
Agomelatine-d₄ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

HY-17038B

Agomelatine (L(+)-Tartaric acid) S-20098 L(+)-Tartaric acid	Melatonin Receptor 5-HT Receptor Endogenous Metabolite	Neurological Disease
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.

HY-17038S2

Agomelatin-d3 S-20098-d₃	Melatonin Receptor 5-HT Receptor Endogenous Metabolite	Neurological Disease
Agomelatin-d₃ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

HY-16687

Eltoprazine DU 28853	5-HT Receptor	Neurological Disease
Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.

HY-15856

cis-(Z)-Flupentixol dihydrochloride cis-(Z)-Flupenthixol dihydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
cis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with K_i values of 0.38 nM and 7 nM for D2 receptor and *5-HT_2A*, respectively.

HY-101324A

MK-212 monohydrochloride CPP monohydrochloride	5-HT Receptor	Neurological Disease
MK-212 (CPP) monohydrochloride is a centrally acting *5-HT_1C/5-HT₂* agonist. MK-212 monohydrochloride can stimulate phosphoinositide hydrolysis in cerebral cortex.

HY-B1371

Spiperone Spiroperidol	Dopamine Receptor 5-HT Receptor	Neurological Disease
Spiperone is a potent dopamine D2, serotonin 5-HT_1A, and serotonin *5-HT_2A* antagonist. Spiperone is a widely used pharmacological tool. Spiperone has the potential for the research of neurology diseases.

HY-B0031S3

Quetiapine-d8 hemifumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine-d₈ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].

HY-N1957

Gamma-Mangostin γ-Mangostin	5-HT Receptor	Metabolic Disease
Gamma-Mangostin is a novel competitive *5-hydroxytryptamine 2A (5-HT2A) receptors* antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 µM) .

HY-B0031S4

Quetiapine hemifumarate-d8	Dopamine Receptor 5-HT Receptor	Neurological Disease
Quetiapine (hemifumarate)-d₈ is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].

HY-B0032S

Lurasidone-d8 hydrochloride SM-13496-d₈ (hydrochloride)	Isotope-Labeled Compounds Dopamine Receptor 5-HT Receptor	Neurological Disease
Lurasidone-d₈ (hydrochloride) is the deuterium labeled Lurasidone, which is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C.

HY-N8200

Cassiaside B2	Phosphatase Monoamine Oxidase 5-HT Receptor	Inflammation/Immunology
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a *5-HT2C* receptor agonist...

HY-A0019A

Paliperidone palmitate 9-Hydroxyrisperidone palmitate	Dopamine Receptor 5-HT Receptor	Neurological Disease
Paliperidone palmitate (9-Hydroxyrisperidone palmitate), an atypical long-acting antipsychotic agent, is an ester proagent of Paliperidone. Paliperidone is a dopamine antagonist and *5-HT2A* antagonist of the atypical antipsychotic class. Paliperidone palmitate shows efficacy against schizophrenia.

HY-133111S

3-Hydroxy agomelatine-d3	5-HT Receptor	Neurological Disease
3-Hydroxy agomelatine-d₃ is a deuterium labeled 3-Hydroxy agomelatine. 3-Hydroxy agomelatine is a 5-HT2C receptor antagonist with an IC50 of 3.2 μM and a Ki of 1.8 μM[1].

HY-A0095S

Flibanserin-d4 BIMT-17-d₄; BIMT-17BS-d₄	5-HT Receptor	Neurological Disease
Flibanserin-d₄ is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].

HY-15296

Cabergoline FCE-21336	Dopamine Receptor Autophagy	Endocrinology Cancer
Cabergoline is an ergot derived-dopamine D₂-like receptor agonist that has high affinity for D₂, D₃, and *5-HT_2B* receptors (K_i=0.7, 1.5, and 1.2, respectively).

HY-101341

RS 67333 hydrochloride	5-HT Receptor	Neurological Disease
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pK_i of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.

HY-14827

Zicronapine Lu 31-130	Dopamine Receptor 5-HT Receptor	Neurological Disease
Zicronapine is an antipsychotic medication with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine has potent antagonistic effects at dopamine D1/D2, and *serotonin 5-HT2A receptors*.

HY-15419

RS-127445 hydrochloride	5-HT Receptor	Neurological Disease
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.

HY-15419A

RS-127445	5-HT Receptor	Neurological Disease
RS-127445 is a selective, high affinity, orally bioavailable 5-HT_2B receptor antagonist with a pK_i of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.

HY-100703A

Pipamperone dihydrochloride Floropipamide dihydrochloride; McN-JR 3345 dihydrochloride; R 3345 dihydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
Pipamperone (Floropipamide; McN-JR 3345) dihydrochloride is a high-affinity antagonist of 5-HT_2A receptor (pK_i=8.2) and D₄ receptor (pK_i=8.0) and a low-affinity antagonist of D₂ receptor (pK_i=6.7).

HY-109112

Brilaroxazine RP5063	Dopamine Receptor 5-HT Receptor	Inflammation/Immunology Neurological Disease
Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (K_i=1.5 nM) and 5-HT2A (K_i=2.5 nM), and has antagonist activity at 5-HT2B (K_i=0.19 nM), and 5-HT7 (K_i=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.

HY-13575A

Blonanserin dihydrochloride AD-5423 dihydrochloride	5-HT Receptor Dopamine Receptor Adrenergic Receptor Sigma Receptor	Neurological Disease
Blonanserin dihydrochloride is a potent and orally active *5-HT_2A* and dopamine D2 receptor antagonist, with K_i values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

HY-101641

NRA-0160	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
NRA-0160 is a selective dopamine D4 receptor antagonist, with a K_i value of 0.48 nM and with negligible affinity for dopamine D2 receptor (K_i: >10000 nM), D3 receptor (K_i: 39 nM), rat 5-HT2A receptor (K_i: 180 nM) and rat α1 adrenoceptor (K_i: 237 nM).

HY-100703

Pipamperone Floropipamide; McN-JR 3345; R 3345	5-HT Receptor Dopamine Receptor	Neurological Disease
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT_2A receptor (pK_i=8.2) and D₄ receptor (pK_i=8.0) and a low-affinity antagonist of D₂ receptor (pK_i=6.7).

HY-14153AS

Tegaserod-13C,d3 maleate SDZ-HTF-919-¹³C,d₃; HTF-919-¹³C,d₃	5-HT Receptor	Metabolic Disease Neurological Disease
Tegaserod-¹³C,d₃ (maleate) is the ¹³C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].

HY-13575

Blonanserin AD-5423	5-HT Receptor Dopamine Receptor Adrenergic Receptor Sigma Receptor	Neurological Disease
Blonanserin (AD-5423) is a potent and orally active *5-HT_2A* (K_i=0.812 nM) and dopamine D2 receptor (K_i=0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.

HY-100851A

LY-272015 hydrochloride	5-HT Receptor	Cardiovascular Disease
LY-272015 hydrochloride is an orally active, specific 5-HT_2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats.

HY-15296S1

Cabergoline-d6 FCE-21336-d₆	Dopamine Receptor Autophagy	Endocrinology
Cabergoline-d₆ is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).

HY-14827A

Zicronapine fumarate Lu 31-130 fumarate	Dopamine Receptor 5-HT Receptor	Neurological Disease
Zicronapine (Lu 31-130) fumarate is an antipsychotic medication with a strong pro-cognitive effect in animal models and the potential to treat a number of neurological and psychiatric diseases. Zicronapine (Lu 31-130) fumarate has potent antagonistic effects at dopamine D1/D2, and *serotonin 5-HT2A receptors*.

HY-15296S

Cabergoline-d5 FCE-21336-d₅	Dopamine Receptor Autophagy	Endocrinology
Cabergoline-d₅ is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].

HY-A0019

Paliperidone 9-Hydroxyrisperidone	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and *5-HT2A* antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.

HY-19733

Lumateperone tosylate ITI-007 tosylate	5-HT Receptor Dopamine Receptor	Neurological Disease
Lumateperone (ITI-007) tosylate is a *5-HT2A* receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

HY-103105A

LP 12 hydrochloride hydrate	5-HT Receptor	Neurological Disease
LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a K_i of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (K_i values are 224 nM, 60.9 nM and >1000 nM, respectively).

HY-17637

Lumateperone ITI-007	Dopamine Receptor 5-HT Receptor	Neurological Disease
Lumateperone (ITI-007) is a *5-HT2A* receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.

HY-B0731

Perospirone hydrochloride SM-9018	5-HT Receptor Dopamine Receptor	Neurological Disease
Perospirone hydrochloride (SM-9018) is an orally active antagonist of *5-HT_2A* receptor (K_i of 0.6 nM) and dopamine D₂ receptor (K_i of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT_1A receptor (K_i of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research.

HY-101369

BW-723C86	5-HT Receptor	Neurological Disease
BW-723C86 is a potent and a selective 5-HT2B receptor agonist. BW-723C86 exhibits anxiolytic-like actions. BW-723C86 also causes hyperphagia and reduced grooming in rats.

HY-14542A

Ziprasidone hydrochloride CP-88059 hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059) hydrochloride is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride has affinities for Rat D₂ (K_i=4.8 nM), *5-HT_2A* (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

HY-103105

LP 12 hydrochloride	5-HT Receptor	Neurological Disease
LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a K_i of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (K_i values are 224 nM, 60.9 nM and >1000 nM, respectively).

HY-17407

Ziprasidone hydrochloride monohydrate CP 88059 hydrochloride monohydrate	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate has affinities for Rat D₂ (K_i=4.8 nM), *5-HT_2A* (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

HY-14542C

Ziprasidone mesylate CP-88059 mesylate	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059) mesylate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate has affinities for Rat D₂ (K_i=4.8 nM), *5-HT_2A* (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

HY-101727

Nexopamil racemate	Calcium Channel 5-HT Receptor	Cardiovascular Disease
Nexopamil racemate is the racemate of Nexopamil. Nexopamil is a combined Ca²⁺/5-HT₂ antagonist on thrombus formation in vivo and on platelet aggregation in vitro.

HY-14542

Ziprasidone CP-88059	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D₂ (K_i=4.8 nM), *5-HT_2A* (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

HY-15780S

Brexpiprazole-d8 OPC-34712-d₈	5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole-d₈ is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2A receptor antagonist (Ki=0.47 nM)[1][2].

HY-14542B

Ziprasidone mesylate trihydrate CP-88059 mesylate trihydrate	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D₂ (K_i=4.8 nM), 5-HT_2A (K_i=0.42 nM) and 5-HT_1A (K_i=3.4 nM).

HY-103428

LE 300	Dopamine Receptor 5-HT Receptor	Neurological Disease
LE 300 is a potent and selective dopamine D1-like receptor antagonist with K_is of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT_2A receptor with a pA2 of 8.32 in a rat tail artery assay.

HY-A0019S

Paliperidone-d4	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Neurological Disease
Paliperidone-d₄ is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia[1].

HY-109118A

Masupirdine mesylate SUVN-502 mesylate	5-HT Receptor	Neurological Disease
Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (K_i of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.

HY-21995

BGC20-761	5-HT Receptor Dopamine Receptor	Neurological Disease
BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptor K_i values: 5-HT6 (20 nM), 5-HT2A (69 nM), D2 (140 nM). BGC20-761, can enhance long-term memory. BGC20-761 has potential utility as an antipsychotic agent.

HY-103110

ST1936	5-HT Receptor Adrenergic Receptor	Neurological Disease
ST1936 is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor.

HY-14557A

Pimavanserin hemitartrate ACP-103 hemitartrate	5-HT Receptor	Neurological Disease
Pimavanserin (ACP-103) hemitartrate is a potent *5-HT 2A* receptor inverse agonist with pIC₅₀ and pK_i of 8.73 and 9.3, respectively.

HY-A0077S1

Perphenazine-d4	Histamine Receptor Dopamine Receptor Autophagy Apoptosis Adrenergic Receptor 5-HT Receptor	Neurological Disease Endocrinology
Perphenazine-d₄ is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.

HY-103110A

ST1936 oxalate	5-HT Receptor Adrenergic Receptor	Neurological Disease
ST1936 oxalate is a selective, nanomolar affinity 5-HT₆ receptor agonist with K_i values of 13 nM, 168 nM and 245 nM for human 5-HT₆, 5-HT₇ and 5-HT_2B receptors, respectively. ST1936 oxalate also shows moderate affinity (K_i of 300 nM) for human and rat α2 adrenergic receptor.

HY-B0731A

Perospirone SM-9018 free base	5-HT Receptor Dopamine Receptor	Neurological Disease
Perospirone (SM-9018 free base) is an orally active antagonist of *5-HT_2A* receptor (K_i=0.6 nM) and dopamine D₂ receptor (K_i=1.4 nM), and also a partial agonist of 5-HT_1A receptor (K_i=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.

HY-145699

UCSF686	5-HT Receptor	Others
UCSF686 is a probe with which to study the function of the 5-HT_5AR. UCSF686 loses affinity at 5-HT_5AR (>10 000 nM) but not at 5-HT_1AR, 5-HT_2BR, and 5-HT₇R. UCSF686 controls for off-target effects.

HY-124591

TC-2153	5-HT Receptor Monoamine Oxidase	Neurological Disease
TC-2153 is a selective inhibitor of striatal-enriched protein tyrosine phosphatase (STEP), with psychotropic activity and low acute toxicity. TC-2153 increases the expression of brain-derived neurotropic factor (BDNF) in the brain. And it decreases MAOA and 5-HT1A receptors mRNA level in midbrain. TC-2153 also inhibits 5-HT2A receptor-mediated signaling.

HY-119209

Nefazodone	5-HT Receptor Cytochrome P450	Inflammation/Immunology Neurological Disease
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT_2A receptors, and moderately inhibit 5-HT and noradrenaline reuptake. Nefazodone can also relieve the adverse effects of stress on the the immune system of mice. Nefazodone has a high affinity for CYP3A4 isoenzyme, which indicates that it has certain risk of agent-agent interaction.

HY-17410A

Iloperidone hydrochloride HP 873 hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Iloperidone hydrochloride (HP 873 hydrochloride) is a *D₂/5-HT₂* receptor antagonist. Iloperidone hydrochloride is an atypical antipsychotic for the schizophrenia symptoms.

HY-17410

Iloperidone HP 873	5-HT Receptor Dopamine Receptor	Neurological Disease
Iloperidone (HP 873) is a *D₂/5-HT₂* receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.

HY-A0077

Perphenazine	Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy	Cancer Endocrinology Inflammation/Immunology Neurological Disease
Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.

HY-A0095A

Flibanserin hydrochloride BIMT-17 hydrochloride; BIMT-17BS hydrochloride	5-HT Receptor	Cancer Neurological Disease
Flibanserin (BIMT-17; BIMT-17BS) hydrochloride is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with K_i values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride binds to dopamine D4 receptors with an K_i value of 4-24 nM. Flibanserin hydrochloride shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research^-.

HY-A0095

Flibanserin BIMT-17; BIMT-17BS	5-HT Receptor	Neurological Disease Cancer
Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with K_i values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an K_i value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research^-.

HY-A0077A

Perphenazine dihydrochloride	Dopamine Receptor Histamine Receptor 5-HT Receptor Adrenergic Receptor Apoptosis Autophagy	Cancer Endocrinology Inflammation/Immunology Neurological Disease
Perphenazine dihydrochloride is an orally active dopamine receptor and histamine-1 receptor antagonist, with K_i values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine dihydrochloride also binds to Alpha-1A adrenergic receptor. Perphenazine dihydrochloride inhibits cancer cell proliferation, and induces apoptosis. Perphenazine dihydrochloride can be used in the research of mental disease, cancer, inflammation.

HY-133152

Brexpiprazole S-oxide DM-3411	5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT_1A and dopamine receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a *5-HT_2A* receptor antagonist with a K_i of 0.47 nM.

HY-A0095S1

Flibanserin-d4-1 BIMT-17-d₄-1; BIMT-17BS-d₄-1	5-HT Receptor	Neurological Disease
Flibanserin-d₄-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].

HY-109118

Masupirdine free base SUVN-502 free base	5-HT Receptor	Neurological Disease
Masupirdine free base (SUVN-502 free base) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (K_i of 2.04 nM for human 5-HT6 receptor). Masupirdine free base (SUVN-502 free base) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.

HY-13575S1

Blonanserin-d5 AD-5423-d₅	5-HT Receptor Dopamine Receptor	Neurological Disease
Blonanserin-d₅ is a deuterium labeled Blonanserin. Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic[1][2].

HY-13575S

Blonanserin D8 AD-5423 d₈	5-HT Receptor Dopamine Receptor	Neurological Disease
Blonanserin-d₈ is a deuterium labeled Blonanserin. Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic[1][2].

HY-18099A

S1RA hydrochloride E-52862 hydrochloride	Sigma Receptor 5-HT Receptor	Neurological Disease
S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a K_i value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (K_i >1000 nM). S1RA hydrochloride is a human *5-HT2B* receptor antagonist with an IC₅₀ value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.

HY-133152S

Brexpiprazole S-oxide-d8 DM-3411 d₈	5-HT Receptor Dopamine Receptor	Neurological Disease
Brexpiprazole S-oxide-d₈ is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].

HY-116941

A-381393	Dopamine Receptor	Neurological Disease
A-381393 is a potent, selective, brain penetrate dopamine D₄ receptor antagonist, with K_is of 1.5, 1.9 and 1.6 nM for human dopamine D_4.4, D_4.2, and D_4.7 receptor, respectively, >2700-fold selectivity over D₁, D₂, D₃ and D₅ dopamine receptors. A-381393 shows moderate affinity for 5-HT_2A (K_i, 370 nM).

HY-15780A

Brexpiprazole hydrochloride OPC-34712 hydrochloride	5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Brexpiprazole (OPC-34712) hydrochloride, an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a *5-HT2A* receptor antagonist with a K_i of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM).

HY-15780

Brexpiprazole OPC-34712	5-HT Receptor Dopamine Receptor Adrenergic Receptor	Neurological Disease
Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a *5-HT2A* receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α_1B (K_i=0.17 nM) and α_2C receptors (K_i=0.59 nM).

HY-103404

PNU-96415E
Dopamine Receptor 5-HT Receptor Neurological Disease

PNU-96415E is a selective D₄/5-HT_2A antagonist. PNU-96415E may have potential antipsychotic efficacy.

HY-17410S

Iloperidone-d3	5-HT Receptor Dopamine Receptor	Neurological Disease
Iloperidone-d₃ is the deuterium labeled Iloperidone. Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms[1][2].

HY-14541S

Olanzapine-d3 LY170053-d₃	5-HT Receptor Dopamine Receptor mAChR Adrenergic Receptor Autophagy Mitophagy Apoptosis	Cancer Neurological Disease
Olanzapine-d₃ is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].

HY-B1371A

Spiperone hydrochloride Spiroperidol hydrochloride	Dopamine Receptor 5-HT Receptor Adrenergic Receptor Chloride Channel	Inflammation/Immunology Neurological Disease
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D₂ receptor (K_i values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D₂, D₃, D₄, D₁ and D₅ receptors, respectively) and 5-HT_2A/5-HT_1A receptor (K_is of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC). Antipsychotic and anti-inflammatory activities.

HY-105285

Piromelatine Neu-P11	Melatonin Receptor 5-HT Receptor P2X Receptor TRP Channel Sodium Channel	Neurological Disease
Piromelatine (Neu-P11) is a melatonin MT₁/MT₂ receptor agonist, serotonin 5-HT_1A/5-HT_1D agonist, and serotonin 5-HT_2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.

HY-15780S1

Brexpiprazole-d8-1 OPC-34712-d₈-1	Dopamine Receptor Adrenergic Receptor 5-HT Receptor	Neurological Disease
Brexpiprazole-d₈-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].

HY-106584

Mosapramine Clospipramine	Dopamine Receptor	Neurological Disease
Mosapramine (Clospipramine) is an orally active and potent dopamine receptor antagonist with high affinity to dopamine receptor subtypes 2, 3 and 4, and with moderate affinity for the 5-HT² receptor. Mosapramine shows antipsychotic activity and can be used in schizophrenia research.

HY-101343

RS 39604	5-HT Receptor	Neurological Disease
RS 39604 is a potent, selective, and orally active 5-HT₄ receptor antagonist with a pK_i of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pK_i<6.5) for 5-HT_1A, 5-HT_2C, 5-HT₃, α_1c, D₁, D₂, M₁, M₂, AT₁, B₁ and opioid mu receptors and moderate affinity for δ₁, (pK_i=6.8) and δ₂ (pK_i=7.8) sites.

HY-105542

Niaprazine	Histamine Receptor	Neurological Disease
Niaprazine is a histamine H1-receptor antagonist. Niaprazine has antihistamine and antiserotonin activities and can be used for sleep disorder research.

HY-B1396

Nefazodone hydrochloride BMY-13754; MJ-13754-1	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Nefazodone hydrochloride (BMY-13754) is a potent and selective *5HT2A* (K_i=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC₅₀ of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.

HY-103430

SKF-83566 hydrobromide	Dopamine Receptor 5-HT Receptor Adenylate Cyclase	Neurological Disease
SKF-83566 hydrobromide is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT₂ receptor (K_i=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC₅₀ of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC₂) over AC₁ and AC₅ in the isolated rabbit thoracic aorta. SKF-83566 can be used for the research of parkinson’s disease and nicotine craving alleviation.

HY-103430A

SKF-83566	Dopamine Receptor 5-HT Receptor Adenylate Cyclase	Neurological Disease
SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT₂ receptor (K_i=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC₅₀ of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC₁ and AC₅ in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.

HY-W050162

(E)-3,4,5-Trimethoxycinnamic acid TMCA	GABA Receptor 5-HT Receptor	Neurological Disease
(E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABA_A/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to *5-HT_2C* and 5-HT_1A receptor, with IC₅₀ values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.

HY-133112

7-Desmethyl-3-hydroxyagomelatine 3-Hydroxy-7-desmethyl agomelatine	Melatonin Receptor 5-HT Receptor	Neurological Disease
7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine), a metabolite of Agomelatine, has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and serotonergic (5HT2C) antagonist.

HY-14147

Renzapride BRL 24924	5-HT Receptor	Metabolic Disease
Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT₄ receptor agonist with a K_i value of 115 nM. Renzapride (BRL 24924) is also a *5HT2b* and 5HT3 receptor antagonist. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study.

HY-136109

SEP-363856 hydrochloride SEP-856 hydrochloride	5-HT Receptor	Neurological Disease
SEP-363856 hydrochloride (SEP-856 hydrochloride), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride (SEP-856 hydrochloride) has the potential for the study of schizophrenia.

HY-136109A

SEP-363856 SEP-856	5-HT Receptor	Neurological Disease
SEP-363856 (SEP-856), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 (SEP-856) has the potential for the study of schizophrenia.

HY-B1396S1

Nefazodone-d6 dihydrochloride BMY-13754-d₆ (dihydrochloride); MJ-13754-1-d₆ (dihydrochloride)	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Nefazodone-d₆ (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

HY-B1396S

Nefazodone-d6 hydrochloride BMY-13754-d₆; MJ-13754-1-d₆	5-HT Receptor Adrenergic Receptor	Neurological Disease Endocrinology
Nefazodone-d₆ (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

HY-14147A

(S)-Renzapride (S)-BRL 24924	5-HT Receptor	Metabolic Disease
(S)-Renzapride ((S)-BRL 24924) is the isomer of HY-14147 Renzapride. Renzapride is a 5-HT₄ receptor agonist with a K_i value of 115 nM. Renzapride also is a *5HT2b* and 5HT3 receptor antagonist. Renzapride can be used for constipation predominant irritable bowel syndrome (C-IBS) study.

HY-134807

Indophagolin	P2X Receptor 5-HT Receptor Autophagy	Cancer
Indophagolin is a potent, indoline-containing autophagy inhibitor (IC₅₀=140 nM). Indophagolin antagonizes the purinergic receptor P2X₄ as well as P2X₁ and P2X₃ with IC₅₀s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the G_q-protein-coupled P2Y₄, P2Y₆, and P2Y₁₁ receptors (IC₅₀s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT₆ (IC₅₀=1.0 μM) and a moderate effect on receptors 5-HT_1B, 5-HT_2B, 5-HT_4e, and 5-HT₇.

HY-136109B

(Rac)-SEP-363856 (Rac)-SEP-856	5-HT Receptor	Neurological Disease
(Rac)-SEP-363856 is the racemate of SEP-363856. SEP-363856（SEP-856）, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 （SEP-856） has the potential for the treatment of schizophrenia.

HY-109067A

Opiranserin hydrochloride VVZ-149 hydrochloride	GlyT 5-HT Receptor P2X Receptor	Neurological Disease
Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain.

HY-109067

Opiranserin VVZ-149	GlyT 5-HT Receptor P2X Receptor	Neurological Disease
Opiranserin (VVZ-149), a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC₅₀s of 0.86 and 1.3 μM, respectively. Opiranserin shows antagonistic activity on rP2X3 (IC₅₀=0.87 μM). Opiranserin is development as an injectable agent for the treatment of postoperative pain.

HY-14539

Clozapine HF 1854	Dopamine Receptor mAChR Adrenergic Receptor 5-HT Receptor	Neurological Disease
Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a K_i of 75 nM. Clozapine inhibits the muscarinic M1 receptor and *serotonin 5HT2A receptor* with K_is of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC₅₀=11 nM).

Cat. No.	Product Name	Target	Category

HY-100971

Spiramide AMI-193	5-HT Receptor Dopamine Receptor	Alkaloids Piperidine Alkaloids Classification of Application Fields Disease Research Fields Neurological Disease Source classification Plants Rosaceae Spiraea japonica
Spiramide (AMI-193) is a potent and selective antagonist of *5-HT₂* and dopamine D2 receptor, with K_is of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT₂ versus 5-HT_1C (K_i=4300 nM) receptors. Spiramide exhibits antipsychotic activity.

HY-N4157

Isopteropodine	mAChR 5-HT Receptor	Terpenoids Iridoids Source classification Plants Rubiaceae Uncaria rhynchophylla (Miq.) Miq. ex Havil.
Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and *5-HT2* receptors.

HY-N0145

Puerarin	5-HT Receptor	Flavonoids Isoflavones Phenols Polyphenols Classification of Application Fields Disease Research Fields Cancer Source classification Plants Leguminosae Pueraria edulis Pampan.
Puerarin, an isoflavone extracted from Radix puerariae, is a *5-HT2C* receptor antagonist.

HY-N0049

Nuciferine	5-HT Receptor Dopamine Receptor	Alkaloids Isoquinoline Alkaloids Source classification Plants other families
Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), *5-HT_2C* (IC₅₀=131 nM), and *5-HT_2B* (IC₅₀=1 μM), an inverse agonist at 5-HT₇ (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and 5-HT₆ (EC₅₀=700 nM), an agonist at 5-HT_1A (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-N0775

Isocorynoxeine 7-Isocorynoxeine	5-HT Receptor	Alkaloids Indole Alkaloids Source classification Plants Rubiaceae Uncaria rhynchophylla (Miq.) Miq. ex Havil.
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of *5-HT_2A* receptor-mediated current response with an IC₅₀ of 72.4 μM.

HY-N0737

Harmine hydrochloride Telepathine hydrochloride	DYRK 5-HT Receptor	Indole Alkaloids Alkaloids Structural Classification Zygophyllaceae Peganum harmala Linn. Plants Source classification
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM.

HY-N0737A

Harmine Telepathine	DYRK 5-HT Receptor	Indole Alkaloids Alkaloids Structural Classification Zygophyllaceae Peganum harmala Linn. Plants Source classification
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT_2A serotonin receptor, with an K_i of 397 nM.

HY-N1957

Gamma-Mangostin γ-Mangostin	5-HT Receptor	Phenols Xanthones Polyphenols Structural Classification Guttiferae Garcinia mangostana Linn. Plants Metabolic Disease Disease Research Fields Classification of Application Fields
Gamma-Mangostin is a novel competitive *5-hydroxytryptamine 2A (5-HT2A) receptors* antagonist, purified from the fruit hull of the medicinal plant Garcinia mangostana. Gamma-Mangostin is a inhibitor of Transthyretin (TTR) fibrillization, it binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3^H] spiperone binding to cultured rat aortic myocytes (IC₅₀=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC₅₀=0.32 µM) .

HY-N8200

Cassiaside B2	Phosphatase Monoamine Oxidase 5-HT Receptor	Phenols Monophenols Classification of Application Fields Disease Research Fields Inflammation/Immunology Source classification Plants Caesalpiniaceae Cassia obtusifolia L.
Cassiaside B2 is a protein tyrosine phosphatase 1B (PTP1B) and human monoamine oxidase A (hMAO-A) inhibitor. Cassiaside B2 possesses antiallergic and is a *5-HT2C* receptor agonist...

HY-A0019

Paliperidone 9-Hydroxyrisperidone	Dopamine Receptor 5-HT Receptor Adrenergic Receptor	Structural Classification Natural Products Endogenous metabolite Source classification
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and *5-HT2A* antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.

Cat. No.	Product Name

HY-14940S

Volinanserin-d4 hydrochloride
Volinanserin-d₄ (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity[1][2].

HY-110232

Risperidone-d4
Risperidone-d₄ is the deuterium labeled Risperidone. Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.

HY-B0352S

Mirtazapine D3
Mirtazapine-d₃ is a deuterium labeled Mirtazapine. Mirtazapine is a 5-HT receptor inhibitor. Mirtazapine is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent by blocking 5-HT2 and 5-HT3 receptors[1].

HY-B1213S

Trimipramine-d3 maleate
Trimipramine-d₃ (maleate) is the deuterium labeled Trimipramine maleate. Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively[1][2].

HY-B0352AS

(S)-Mirtazapine-d3
(S)-Mirtazapine-d₃ is a deuterium labeled (S)-Mirtazapine. (S)-Mirtazapine is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception.(S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2[1].

HY-B0352S2

Mirtazapine-d4
Mirtazapine-d₄ is deuterium labeled Mirtazapine. Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively[1][2].

HY-10564S

Sarpogrelate-d3 hydrochloride

Sarpogrelate-d₃ (hydrochloride) is the deuterium labeled Sarpogrelate hydrochloride. Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis[1][2][3].

HY-B0781S

Promethazine-d4 hydrochloride
Promethazine-d₄ (hydrochloride) is the deuterium labeled Promethazine hydrochloride. Promethazine hydrochloride is the first-generation antihistamine; strong antagonist of the H1 receptor and moderate mACh receptor antagonist, moderate affinity for 5-HT2A, 5-HT2C, D2 and α1-adrenergic receptors.

HY-14264S

Cyamemazine-d6
Cyamemazine-d₆ is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity[1][2].

HY-113008AS

cis-Urocanic acid-13C3
cis-Urocanic acid-¹³C₃ is the ¹³C-labeled cis-Urocanic acid. cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor[1].

HY-32329S

Setiptiline-d3

Setiptiline-d₃ is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].

HY-126057S

(R)-Praziquantel-d11
(R)-Praziquantel-d₁₁ is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer[1].

HY-B0031S2

Quetiapine-d8 fumarate

Quetiapine-d₈ (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1][2].

HY-17038S1

Agomelatine-d4
Agomelatine-d₄ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

HY-17038S2

Agomelatin-d3
Agomelatin-d₃ is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively[1]. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively[2].

HY-B0031S3

Quetiapine-d8 hemifumarate

Quetiapine-d₈ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[1].

HY-B0031S4

Quetiapine hemifumarate-d8

Quetiapine (hemifumarate)-d₈ is the deuterium labeled Quetiapine hemifumarate[1]. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects[2].

HY-B0032S

Lurasidone-d8 hydrochloride

Lurasidone-d₈ (hydrochloride) is the deuterium labeled Lurasidone, which is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C.

HY-133111S

3-Hydroxy agomelatine-d3
3-Hydroxy agomelatine-d₃ is a deuterium labeled 3-Hydroxy agomelatine. 3-Hydroxy agomelatine is a 5-HT2C receptor antagonist with an IC50 of 3.2 μM and a Ki of 1.8 μM[1].

HY-A0095S

Flibanserin-d4

Flibanserin-d₄ is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM)[1].

HY-14153AS

Tegaserod-13C,d3 maleate
Tegaserod-¹³C,d₃ (maleate) is the ¹³C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].

HY-15296S1

Cabergoline-d6
Cabergoline-d₆ is deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).

HY-15296S

Cabergoline-d5
Cabergoline-d₅ is the deuterium labeled Cabergoline. Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively)[1][2].

HY-15780S

Brexpiprazole-d8
Brexpiprazole-d₈ is a deuterium labeled Brexpiprazole (OPC-34712). Brexpiprazole, an atypical antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine receptor (Ki=0.12 nM and 0.3 nM, respectively). Brexpiprazole is also a 5-HT2A receptor antagonist (Ki=0.47 nM)[1][2].

HY-A0019S

Paliperidone-d4
Paliperidone-d₄ is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia[1].

HY-A0077S1

Perphenazine-d4
Perphenazine-d₄ is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.

HY-A0095S1

Flibanserin-d4-1

Flibanserin-d₄-1 is deuterium labeled Flibanserin. Flibanserin (BIMT-17) is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM). Flibanserin binds to dopamine D4 receptors (4-24 nM), and has negligible affinity for a variety of other neurotransmitter receptors and ion channels. Flibanserin is efficacious in treating hypoactive sexual desire disorder (HSDD)[1][2].

HY-13575S1

Blonanserin-d5

Blonanserin-d₅ is a deuterium labeled Blonanserin. Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic[1][2].
HY-13575S

Blonanserin D8

Blonanserin-d₈ is a deuterium labeled Blonanserin. Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic[1][2].

HY-133152S

Brexpiprazole S-oxide-d8

Brexpiprazole S-oxide-d₈ is a deuterium labeled Brexpiprazole S-oxide. Brexpiprazole S-oxide is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM[1][2][3].

HY-17410S

Iloperidone-d3
Iloperidone-d₃ is the deuterium labeled Iloperidone. Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms[1][2].

HY-14541S

Olanzapine-d3
Olanzapine-d₃ is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic[1][2].

HY-15780S1

Brexpiprazole-d8-1

Brexpiprazole-d₈-1 is the deuterium labeled Brexpiprazole[1]. Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM)[2][3].

HY-B1396S1

Nefazodone-d6 dihydrochloride
Nefazodone-d₆ (dihydrochloride) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

HY-B1396S

Nefazodone-d6 hydrochloride
Nefazodone-d₆ (hydrochloride) is the deuterium labeled Nefazodone hydrochloride. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity[1][2].

5-HT2

Inhibitors & Agonists

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Isotope-Labeled Compounds

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