Search Result
Results for "
5-HT2
" in MedChemExpress (MCE) Product Catalog:
36
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-156533
-
|
5-HT Receptor
|
Cancer
|
5-HT2 agonist-1 (Compound 24) is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .
|
-
-
- HY-U00365
-
-
-
- HY-156533A
-
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
5-HT2 agonist-1 (Compound 24) free base is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .
|
-
-
- HY-145841
-
|
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-HT2A, 5-HT2B, and 5-HT2C with EC50 values of 1.7, 0.58, and 0.50 nM, respectively .
|
-
-
- HY-156534
-
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC50s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders .
|
-
-
- HY-156532
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT2C agonist-3 ((+)-19) is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 has antipsychotic drug-like activity. 5-HT2C agonist-3 blocks Amphetamine-induced hyperactivity .
|
-
-
- HY-147203
-
|
5-HT Receptor
|
Cardiovascular Disease
Metabolic Disease
Endocrinology
Cancer
|
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-153912
-
|
5-HT Receptor
|
Others
|
5-HT2A receptor agonist-3 is the most selective agonist for the human 5-HT2A receptor yet discovered, with a Ki of 2.5 nM, and with 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor .
|
-
-
- HY-162176
-
-
-
- HY-U00286
-
|
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-157425
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT2CR agonist 1 (compound 8), a 7-chloro analogue, is a selective 5-HT2CR partial agonist (Emax=71.09%) with an EC50 value of 121.5 nM and no observed activity toward 5-HT2AR or 5-HT2BR. 5-HT2CR agonist 1 exhibits no recruitment activity for β-arrestin and shows low inhibition of hERG at 10 μM .
|
-
-
- HY-156532A
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT2C agonist-3 ((+)-19) free base is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 free base has antipsychotic drug-like activity. 5-HT2C agonist-3 free base blocks Amphetamine-induced hyperactivity .
|
-
-
- HY-161247
-
|
5-HT Receptor
|
Metabolic Disease
|
5HT2A antagonist 2 is an orally active, selective antagonist for 5HT2A with IC50 of 14 nM. 5-HT2A antagonist 2 exhibits good chemical, hepatocyte, and plasma stability, without significant cytotoxicity in cell lines VERO, HFL-1, L929, NIH3T3, CHO-K1 .
|
-
-
- HY-121301
-
|
5-HT Receptor
|
Neurological Disease
|
Amperozide is an atypical antipsychotic that acts as an antagonist of the 5-HT2 receptor with a Ki value of 26 nM. Amperozide has a low affinity for D2 receptors .
|
-
-
- HY-103104
-
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 Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor .
|
-
-
- HY-103148
-
|
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
-
|
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
-
-
-
- HY-100943
-
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 Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki 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-123206
-
|
5-HT Receptor
|
Inflammation/Immunology
|
R-96544 (free base) is a potent, selective and competitive 5-HT2 receptor antagonist. R-96544 (free base) inhibits platelet aggregation induced by serotonin, and inhibits 5-HT2A receptor-mediated contraction of guinea pig trachea .
|
-
-
- HY-125641
-
|
5-HT Receptor
Adrenergic Receptor
|
Cardiovascular Disease
|
AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent .
|
-
-
- HY-10563
-
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)-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-151596
-
-
-
- HY-B0352
-
-
-
- HY-101632
-
-
-
- HY-14940
-
MDL100907; M 100907
|
5-HT Receptor
|
Neurological Disease
|
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.
|
-
-
- HY-132225
-
|
5-HT Receptor
|
Inflammation/Immunology
|
SB 206553 is a 5-HT2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B) and 7.8 nM (5-HT2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders .
|
-
-
- HY-103116
-
-
-
- HY-B1737
-
R 47465
|
|
|
Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity .
|
-
-
- HY-100971
-
AMI-193
|
|
|
Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity .
|
-
-
- HY-14940A
-
(S)-MDL100907; (S)-M 100907
|
5-HT Receptor
|
Neurological Disease
|
(S)-Volinanserin is an isform of Volinanserin (HY-14940). 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.
|
-
-
- HY-14940S
-
MDL100907-d4 hydrochloride; M 100907-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
-
-
-
- HY-116606
-
-
-
- HY-145862
-
-
-
- HY-11018
-
-
-
- HY-11018A
-
-
-
- HY-146076
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research .
|
-
-
- HY-146077
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties .
|
-
-
- HY-B0115A
-
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-HT1C binding site.
|
-
-
- HY-113643
-
|
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-10562
-
-
-
- HY-N4157
-
|
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-11018B
-
-
-
- HY-B1107
-
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
-
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-117646
-
-
-
- HY-135194
-
|
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 Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively .
|
-
-
- HY-U00367
-
-
- HY-101094
-
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-HT1A agonist, with Kis 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 pKi of 7.60 and 8.08 for h5-HT1A.
|
-
- HY-10562A
-
-
- HY-N4156
-
|
Others
|
Others
|
Pteropodine (compound 3) is a monoterpenoid oxindole alkaloid that can be isolated from Hamelia patens. Pteropodine modulates the functions of M1 muscarinic and 5-HT2 receptors. Pteropodine has antioxidant and antimutagenic properties .
|
-
- HY-119156
-
|
5-HT Receptor
|
Others
|
Altanserin can synthesize Fluorine-18 Altanserin. Fluorine-18 Altanserin binds to the brain 5HT2 receptors .
|
-
- HY-B2089
-
|
|
|
Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a 5-HT2 and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research .
|
-
- HY-11018S2
-
R 64 766-d6
|
5-HT Receptor
Dopamine Receptor
P-glycoprotein
|
Neurological Disease
|
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). 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
-
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
-
-
- HY-44132
-
RS 42358-197
|
5-HT Receptor
|
Neurological Disease
|
Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors .
|
-
- HY-B1213S
-
|
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)-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-B1213
-
|
5-HT Receptor
Bacterial
|
Neurological Disease
|
Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, 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-14325
-
|
Dopamine Receptor
|
Neurological Disease
|
L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-14325B
-
|
Dopamine Receptor
|
Neurological Disease
|
L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-14325A
-
|
|
|
L-745870 trihydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 trihydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors .
|
-
- HY-105034
-
BMY 13859-1 free base
|
5-HT Receptor
|
Neurological Disease
|
Tiospirone is a 5-HT2 receptor antagonist with affinity for D2, 5-HT1a, and 5-HT7, and sigma receptors. Tiospirone decreases consumption of ethanol while increasing food intake of rats. Tiospirone can also reduce the reinforcing properties of Cocaine exhibited in the conditioned place preference paradigm .
|
-
- HY-101009
-
Metitepine maleate; Ro-8-6837 maleate
|
|
|
Methiothepin maleate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
|
-
- HY-19686
-
TVX Q 7821 free base
|
|
|
Ipsapirone (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function .
|
-
- HY-124117
-
|
5-HT Receptor
|
Neurological Disease
|
LY 278584 is a potent, highly selective 5-HT3 receptor antagonist with a Ki of 1.62 nM. LY 278584 has no activity on 5-HT1A, 5-HT1B, 5-HT1C, 5-HT1D, or 5-HT2 receptors .
|
-
- HY-107836
-
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 pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
|
-
- HY-19545A
-
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 Kis 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-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
|
-
- HY-108400
-
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 Kis 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-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 maleate also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 maleate inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM .
|
-
- HY-19358
-
2-Methyl-5-hydroxytryptamine; 2-Methylserotonin; 2-Me-5-HT
|
|
|
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-12697A
-
|
Dopamine Receptor
|
Neurological Disease
|
NGB 2904 hydrochloride is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 hydrochloride shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 hydrochloride antagonizes Quinpirole-stimulated mitogenesis .
|
-
- HY-12697
-
|
Dopamine Receptor
|
Neurological Disease
|
NGB 2904 is a potent, selective, orally active and brain-penetrated antagonist of dopamine D3 receptor, with a Ki of 1.4 nM. NGB 2904 shows selectivity for D3 over D2, 5-HT2, α1, D4, D1 and D5 receptors (Kis=217, 223, 642, >5000, >10000 and >10000 nM, respectively). NGB 2904 antagonizes Quinpirole-stimulated mitogenesis .
|
-
- HY-103151
-
|
5-HT Receptor
|
Neurological Disease
|
CP94253 hydrochloride is a potent and selective agonist of 5-HT1B receptor (Ki= 2 nM in a radioligand binding assay).Ki values for 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors are 89, 49, 860, and 1600 nM respectively . CP94253 hydrochloride is centrally active upon systemic administration in vivo .
|
-
- HY-B0352S2
-
-
- HY-12706
-
-
- HY-B0352R
-
Org3770 (Standard); 6-Azamianserin (Standard)
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Mirtazapine (Standard) is the analytical standard of Mirtazapine. This product is intended for research and analytical applications. 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 .
|
-
- HY-B1213A
-
|
|
|
Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, 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-103413
-
|
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 Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. Antipsychotic agent .
|
-
- HY-14541
-
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 (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 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-103094
-
|
5-HT Receptor
|
Inflammation/Immunology
|
LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression .
|
-
- HY-103120
-
|
5-HT Receptor
|
Neurological Disease
|
Org37684 is a highly potent 5-HT2C receptor agonist (pEC50=8.17). Org37684 exhibits a rank order of potency of 5-HT2C>5-HT2B>5-HT2A. 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-HT2A (pEC50=7.11) receptor .
|
-
- HY-101250
-
MDL11939
|
|
|
Glemanserin (MDL11939) is a potent and selective antagonist for serotonin receptor 5-HT2A (Ki=2.89, 0.54 and 2.5 nM for rat 5-HT2A, rabbit 5-HT2A and human 5-HT2A, respectively) .
|
-
- HY-103129A
-
|
5-HT Receptor
|
Neurological Disease
|
SB-200646 is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646 is orally active and has electrophysiological and anxiolytic properties in vivo .
|
-
- HY-103129
-
|
5-HT Receptor
|
Neurological Disease
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo .
|
-
- HY-18596
-
|
5-HT Receptor
|
Neurological Disease
|
SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively . SB-215505 increases wakefulness and motor activity in rats .
|
-
- HY-103155
-
|
5-HT Receptor
|
Neurological Disease
|
SB 221284 is a selective 5-HT2C/2B receptor antagonist with pKi values are 6.4, 7.9 and 8.6 for 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. SB 221284 can be used for the research of neurological disease .
|
-
- HY-103135
-
|
5-HT Receptor
|
Neurological Disease
|
SB 206553 hydrochloride is a high affinity, selective and orally active 5-HT2B / 5-HT2C receptor antagonist (rat 5-HT2B pA2 = 8.89, human 5-HT2C pKi = 7.92) . SB 206553 possesses anxiolytic-like properties .
|
-
- HY-10792
-
SR-46349
|
5-HT Receptor
|
Neurological Disease
|
Eplivanserin (SR-46349) is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
|
-
- HY-103154
-
|
5-HT Receptor
|
Neurological Disease
|
SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects .
|
-
- HY-21994
-
|
5-HT Receptor
|
Neurological Disease
|
Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model .
|
-
- HY-103144
-
|
5-HT Receptor
|
Neurological Disease
|
WAY 629 hydrochloride is a potent and selective 5-HT2C agonist with EC50s of 426, 260000 nM for 5-HT2C and 5-HT2A, respectively. WAY 629 hydrochloride decreases feeding behavior .
|
-
- HY-110129
-
SR-46349 hemifumarate; SR 46349B
|
5-HT Receptor
|
Neurological Disease
|
Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C .
|
-
- HY-W380450
-
Viloxazin; Emovit
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
Viloxazine (Viloxazin) is a norepinephrine reuptake inhibitor, also a potent 5-HT2C agonist and 5-HT2B antagonist with an EC50 of 32 μM and an IC50 of 27 μM for 5-HT2C and 5-HT2B, respectively. The mechanism of action of Viloxazine predominantly involves serotonergic and noradrenergic pathways. Viloxazine can be used for researching depression .
|
-
- HY-119103
-
|
5-HT Receptor
|
Neurological Disease
|
PF-03246799 (PF-3246799) is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research .
|
-
- HY-101630
-
EGIS-3886
|
5-HT Receptor
|
Neurological Disease
|
Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
|
-
- HY-103138A
-
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects .
|
-
- HY-103138
-
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
(Rac)-WAY-161503 hydrochloride is a potent, selective, high affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 hydrochloride displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 hydrochloride has anti-obesity and antidepressant effects .
|
-
- HY-10559
-
APD125
|
5-HT Receptor
|
Neurological Disease
Cancer
|
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
|
-
- HY-125784
-
Viloxazin hydrochloride; Emovit hydrochloride
|
Others
|
Neurological Disease
|
Viloxazine hydrochloride is the hydrochloride salt form of Viloxazine (HY-W380450). Viloxazine (Viloxazin) hydrochloride is a norepinephrine reuptake inhibitor and a potent 5-HT2C agonist agent and 5-HT2B antagonist, EC50 for 5-HT2C b> is 32 μM, and the IC50 for 5-HT2B is 27 μM. Viloxazine hydrochloride's mechanism of action primarily involves serotonergic and noradrenergic pathways. Viloxazine hydrochloride is used in antidepressant research .
|
-
- HY-117118A
-
-
- HY-101365
-
|
5-HT Receptor
|
Neurological Disease
|
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=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
-
|
5-HT Receptor
|
Neurological Disease
|
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=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-100330
-
|
|
|
YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
|
-
- HY-103115
-
EMD 281014; LY 2422347 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
Pruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT2A receptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2A receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia .
|
-
- HY-133024
-
|
5-HT Receptor
|
Neurological Disease
|
Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor. Flumexadol is an orally active non-narcotic analgesic .
|
-
- HY-100970
-
|
|
|
4F 4PP (oxalate) is a selective 5-HT2A antagonist with almost as high affinity (Ki= 5.3 nM) as ketanserin but with a much lower affinity for 5-HT2C sites (Ki= 620 nM) .
|
-
- HY-10564
-
MCI-9042
|
5-HT Receptor
|
Cardiovascular Disease
|
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 .
|
-
- HY-14153
-
|
5-HT Receptor
Apoptosis
|
Metabolic Disease
Cancer
|
Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C 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-14546
-
OPC-14597
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
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-118152
-
|
5-HT Receptor
|
Neurological Disease
|
Org-12962 is a potent, selective and orally active 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively .Org-12962 displays antiaversive effects in a rat model of panic-like anxiety .
|
-
- HY-14546A
-
OPC-14597 monohydrate
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
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-14543
-
-
- HY-113008A
-
(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 (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor .
|
-
- HY-10560
-
-
- HY-19469
-
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-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
|
-
- HY-14264
-
|
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 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity .
|
-
- HY-155672
-
|
5-HT Receptor
|
Neurological Disease
|
JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease .
|
-
- HY-B1033
-
|
5-HT Receptor
Dopamine Receptor
Sodium Channel
|
Neurological Disease
|
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki 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
-
SDZ-HTF-919; HTF-919
|
5-HT Receptor
Apoptosis
|
Neurological Disease
Metabolic Disease
|
Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C 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
-
MCI-9042-d3
|
Isotope-Labeled Compounds
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-B0781
-
|
Histamine Receptor
mAChR
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors .
|
-
- HY-101755
-
-
- HY-N0145
-
-
- HY-123829
-
-
- HY-163205
-
-
- HY-B1101
-
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-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-B1101A
-
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-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively .
|
-
- HY-14546R
-
OPC-14597 (Standard)
|
5-HT Receptor
Dopamine Receptor
|
Infection
Neurological Disease
Inflammation/Immunology
|
Aripiprazole (Standard) is the analytical standard of Aripiprazole. This product is intended for research and analytical applications. 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-B0781S
-
|
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-19417A
-
|
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 Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively, and has potent antidepressant activity.
|
-
- HY-103140
-
-
- HY-19417
-
|
Serotonin Transporter
5-HT Receptor
|
Neurological Disease
|
Wf-516 hydrochloride is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively.Wf-516 hydrochloride has potent antidepressant activity.
|
-
- HY-15401
-
|
5-HT Receptor
|
Cancer
|
WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a Ki of 10.5±1.1 nM.
|
-
- HY-103153
-
-
- HY-106143
-
-
- HY-14264S
-
|
Isotope-Labeled Compounds
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-111200
-
-
- HY-100171
-
-
- HY-118450
-
-
- HY-103093
-
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
Dopamine Receptor
|
Neurological Disease
|
Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds 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-113008AS
-
(Z)-Urocanic acid-13C3; cis-UCA-13C3
|
Isotope-Labeled Compounds
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
-
-
- HY-156601
-
|
Others
|
Others
|
Bexicaserin (Compound 3) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related diseases .
|
-
- HY-15543A
-
|
5-HT Receptor
|
Neurological Disease
|
CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A 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
-
|
5-HT Receptor
|
Neurological Disease
|
CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A 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-101619
-
-
- HY-101815
-
-
- HY-141422A
-
-
- HY-156601A
-
-
- HY-155117
-
-
- HY-N0049
-
|
Parasite
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (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-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
|
-
- HY-103112
-
|
5-HT Receptor
|
Neurological Disease
|
SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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-103152
-
-
- HY-103112A
-
|
5-HT Receptor
|
Neurological Disease
|
SB 243213 dihydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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
-
|
5-HT Receptor
|
Neurological Disease
|
SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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-10457A
-
TD-5108 hydrochloride
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease .
|
-
- HY-10457
-
TD-5108
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
Velusetrag (TD-5108) is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag can be used for the research of gastrointestinal diseases and Parkinson's disease .
|
-
- HY-149247
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Antipsychotic agent-2 (Compound 11) is a potent antipsychotic agent. Antipsychotic agent-2 shows affinities for 5-HT1A, 5-HT2A, 5-HT2C, D2 and H1 receptors with Kis of 56.6, 66.7, 552, 596 and 1140 nM, respectively. Antipsychotic agent-2 has BBB permeability .
|
-
- HY-N0775
-
7-Isocorynoxeine
|
5-HT Receptor
|
Neurological Disease
|
Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
|
-
- HY-103136
-
-
- HY-N0737
-
Telepathine hydrochloride
|
DYRK
5-HT Receptor
|
Neurological Disease
Cancer
|
Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM .
|
-
- HY-123838
-
-
- HY-N0049R
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (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-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
|
-
- HY-32329
-
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-16729A
-
YKP10811 hydrochloride
|
5-HT Receptor
|
Inflammation/Immunology
|
Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility .
|
-
- HY-101690
-
-
- HY-135392
-
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 pKd of 8.73 and 9.3, respectively.
|
-
- HY-155206
-
|
5-HT Receptor
|
Neurological Disease
|
(+)-OSU6162 is an stabilizer on dopaminergic and serotonergic brain signaling. (+)-OSU6162 is a partial agonist of 5-HT2A receptor. (+)-OSU6162 can be used for neurological research .
|
-
- HY-32329A
-
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-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
|
-
- HY-106136
-
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 Kis of 0.081 nM and 0.042 nM, respectively. TIK-301 is also a 5-HT2B/5-HT2C receptors antagonist with antidepressant action. TIK-301 has the potential for sleep disorders and other circadian rhythm disorders treatment .
|
-
- HY-19283
-
|
|
|
DU125530 is a potent and selective5-HT1A receptor antagonist with Ki 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-15472
-
|
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
-
|
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-15472A
-
|
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-116524
-
|
5-HT Receptor
|
Neurological Disease
|
PF-04781340 is a potent and selective 5-HT2C receptor agonist. PF-04781340 is orally available and have central nervous system penetrant profile .
|
-
- HY-10792A
-
-
- HY-133111
-
|
5-HT Receptor
|
Neurological Disease
|
3-Hydroxy agomelatine is a metabolite of Agomelatine. 3-Hydroxy agomelatine is a 5-HT2C receptor antagonist with an IC50 of 3.2 μM and a Ki of 1.8 μM .
|
-
- HY-118557
-
S-MPEC
|
5-HT Receptor
|
Inflammation/Immunology
|
Iferanserin (S-MPEC) is a selective 5-HT receptor (serotonin receptor) antagonist with an affinity for 5-HT2A receptor. Iferanserin has the potential for internal hemorrhoid disease treatment .
|
-
- HY-101630A
-
EGIS-3886 fumarate
|
5-HT Receptor
|
Others
|
Deramciclane fumarate is an antagonist of 5-HT Receptor. Deramciclane fumarate is an inverse agonist of 5-HT2C Receptor with an IC50 of 168 nM. Deramciclane fumarate also decreases basal phosphoinositide hydrolysis .
|
-
- HY-B0031
-
|
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 pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
- HY-17038
-
S-20098
|
Melatonin Receptor
5-HT Receptor
Endogenous Metabolite
|
Neurological Disease
|
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 . 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 .
|
-
- HY-14544
-
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 pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .
|
-
- HY-17038A
-
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 Kis 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 pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
|
-
- HY-10895
-
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 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi 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-B0366A
-
|
5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
Cancer
|
Cyproheptadine hydrochloride is a potent and orally active 5-HT2A 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
-
|
5-HT Receptor
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
Cyproheptadine is a potent and orally active 5-HT2A 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
-
|
5-HT Receptor
|
Cancer
|
PF-4479745 is a potent and selective 5-HT2C receptor agonist (EC50: 10 nM, ki: 15 nM). PF-4479745 can be used in the research of cardiovascular disease like hypertension .
|
-
- HY-N0737A
-
Harmine
Maximum Cited Publications
17 Publications Verification
Telepathine
|
|
|
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-HT2A serotonin receptor, with an Ki of 397 nM .
|
-
- HY-103147
-
CU32-085 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Mesulergine (CU32-085) hydrochloride is a potent 5-HT2C antagonist and dopamine (DA) agonist. Mesulergine hydrochloride presentes hyperphagia. Mesulergine hydrochloride has the potential for the research of cognitive processes .
|
-
- HY-10895A
-
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 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi 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-13409
-
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C 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-HT2A 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
-
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
SB 242084 dihydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C 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-HT2A 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-32329S
-
|
Isotope-Labeled Compounds
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-17038B
-
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 Kis 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 pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .
|
-
- HY-100794
-
|
|
|
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-101324
-
CPP
|
|
|
MK-212 (CPP) is a centrally acting 5-HT1C/5-HT2 agonist. MK-212 can stimulate phosphoinositide hydrolysis in cerebral cortex .
|
-
- HY-103139
-
|
Others
|
Metabolic Disease
|
Altanserin is a 5-hydroxytryptamine (5-HT2A ) selective radioligand. Altanserin delivers human serotonin. Altanserin can be used to study the biochemical and cellular mechanisms of vulnerability to extracellular 5-HT increase .
|
-
- HY-103403
-
PNU96391 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
(-)-OSU6162 (PNU96391) hydrochloride is a dopamine stabilizer. (-)-OSU6162 hydrochloride acts as partial agonist at 5-HT2A and is a dopamine D2 antagonist. (-)-OSU6162 hydrochloride can be used for the research of aggression and irritability .
|
-
- HY-126057S
-
|
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-15856
-
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 Ki values of 0.38 nM and 7 nM for D2 receptor and 5-HT2A, respectively .
|
-
- HY-B0031S2
-
|
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-17038S1
-
S-20098-d4
|
Isotope-Labeled Compounds
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-17038S2
-
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-101324A
-
CPP monohydrochloride
|
|
|
MK-212 (CPP) monohydrochloride is a centrally acting 5-HT1C/5-HT2 agonist. MK-212 monohydrochloride can stimulate phosphoinositide hydrolysis in cerebral cortex .
|
-
- HY-B1371
-
Spiroperidol
|
|
|
Spiperone is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is a widely used pharmacological tool. Spiperone has the potential for the research of neurology diseases .
|
-
- HY-A0019A
-
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-N8200
-
-
- HY-B0031S3
-
|
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-B0031S4
-
|
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-B0031R
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. 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 .
|
-
- HY-16687
-
DU 28853
|
5-HT Receptor
|
Neurological Disease
|
Eltoprazine (DU 28853) is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine shows antiaggressive and anxiogenic effects .
|
-
- HY-16687A
-
DU 28853 hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
Eltoprazine (DU 28853) hydrochloride is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine hydrochloride shows antiaggressive and anxiogenic effects .
|
-
- HY-B0032S
-
-
- HY-16687B
-
DU 28853 dihydrochloride
|
5-HT Receptor
|
Neurological Disease
|
Eltoprazine (DU 28853) dihydrochloride is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine dihydrochloride shows antiaggressive and anxiogenic effects .
|
-
- HY-15296
-
-
- HY-133111S
-
|
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
-
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-128386
-
-
- HY-101341
-
|
5-HT Receptor
|
Neurological Disease
|
RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi 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-15419
-
|
5-HT Receptor
|
Neurological Disease
|
RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi 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 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
|
-
- HY-14827
-
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-13575A
-
AD-5423 dihydrochloride
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Sigma Receptor
|
Neurological Disease
|
Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki 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-100703A
-
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-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7) .
|
-
- HY-109112
-
RP5063
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
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 (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=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-117046A
-
|
5-HT Receptor
Histamine Receptor
Adrenergic Receptor
|
Neurological Disease
|
AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, and multiple sclerosis .
|
-
- HY-101641
-
-
- HY-100703
-
Floropipamide; McN-JR 3345; R 3345
|
|
|
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7) .
|
-
- HY-13575
-
-
- HY-100851A
-
|
|
|
LY-272015 hydrochloride is an orally active, specific 5-HT2B 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-N1957
-
γ-Mangostin
|
5-HT Receptor
COX
Transthyretin (TTR)
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
Gamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin 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). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes .
|
-
- HY-14153AS
-
SDZ-HTF-919-13C,d3; HTF-919-13C,d3
|
Isotope-Labeled Compounds
5-HT Receptor
|
Neurological Disease
Metabolic 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-15296S1
-
-
- HY-A0019
-
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-17407
-
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 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-14542A
-
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 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-19733
-
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-15296S
-
-
- HY-101369
-
|
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-14542C
-
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 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-17637
-
ITI-007
|
|
|
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-14827A
-
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-157429
-
|
5-HT Receptor
|
Neurological Disease
|
25N-N1-Nap (compound 16) is a β-arrestin-biased 5-HT2A agonist. 25N-N1-Nap antagonizes phencyclidine induced hyperactivity in Male C57BL/6?J mice .
|
-
- HY-B0731
-
SM-9018
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Perospirone hydrochloride (SM-9018) is an orally active antagonist of 5-HT2A receptor (Ki of 0.6 nM) and dopamine D2 receptor (Ki of 1.4 nM). Perospirone hydrochloride is also a partial agonist of 5-HT1A receptor (Ki of 2.9 nM). Perospirone hydrochloride is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
|
-
- HY-14542B
-
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 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-103105A
-
|
5-HT Receptor
|
Neurological Disease
|
LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively) .
|
-
- HY-112538
-
1-NP hydrochloride; 1-NapHThylpiperazine hydrochloride
|
5-HT Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
1-1-Naphthylpiperazine hydrochloride (1-NP hydrochloride; 1-Naphthylpiperazine hydrochloride) is a serotonergic derivative of quipazine, which is both an agonist for 5-HT1A receptor and an antagonist for 5-HT2A receptor. 1-1-Naphthylpiperazine hydrochloride induces cell apoptosis. 1-1-Naphthylpiperazine hydrochloride prevents the immunosuppression and photocarcinogenesis .
|
-
- HY-14542
-
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 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-103428
-
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis 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-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay .
|
-
- HY-103105
-
|
5-HT Receptor
|
Neurological Disease
|
LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively) .
|
-
- HY-101727
-
-
- HY-15780S
-
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-109118A
-
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 (Ki 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
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
BGC20-761 is a selecvtive 5-HT6 and dopamine receptor antagonist (human receptor Ki 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
1 Publications Verification
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-A0019S
-
|
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-B0731A
-
SM-9018 free base
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research .
|
-
- HY-103110A
-
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor .
|
-
- HY-17410
-
-
- HY-17410A
-
-
- HY-14557A
-
ACP-103 hemitartrate
|
5-HT Receptor
|
Neurological Disease
|
Pimavanserin (ACP-103) hemitartrate is a potent 5-HT 2A receptor inverse agonist with pIC50 and pKi of 8.73 and 9.3, respectively.
|
-
- HY-A0077
-
-
- HY-A0077S1
-
|
5-HT Receptor
Adrenergic Receptor
Apoptosis
Autophagy
Dopamine Receptor
Histamine 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-133152
-
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-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 .
|
-
- HY-145699
-
|
5-HT Receptor
|
Others
|
UCSF686 is a probe with which to study the function of the 5-HT5AR. UCSF686 loses affinity at 5-HT5AR (>10 000 nM) but not at 5-HT1AR, 5-HT2BR, and 5-HT7R. UCSF686 controls for off-target effects .
|
-
- HY-A0077A
-
-
- HY-119209
-
|
5-HT Receptor
Cytochrome P450
|
Neurological Disease
Inflammation/Immunology
|
Nefazodone is an orally active phenylpiperazine antidepressant. Nefazodone can potently and selectively block postsynaptic 5-HT2A 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-124591
-
|
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-A0095
-
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 Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research - .
|
-
- HY-109118
-
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 (Ki 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-110024
-
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
S-14506 hydrochloride is a potent 5-HT1A agonist, as well as 5-HT2A/2C antagonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent .
|
-
- HY-A0095A
-
BIMT-17 hydrochloride; BIMT-17BS hydrochloride
|
5-HT Receptor
|
Neurological Disease
Cancer
|
Flibanserin (BIMT-17; BIMT-17BS) hydrochloride is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride binds to dopamine D4 receptors with an Ki 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-A0095S1
-
BIMT-17-d4-1; BIMT-17BS-d4-1
|
Isotope-Labeled Compounds
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-13575S
-
-
- HY-13575S1
-
-
- HY-15780
-
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 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) .
|
-
- HY-18099A
-
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 Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >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-116941
-
|
Dopamine Receptor
|
Neurological Disease
|
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM) .
|
-
- HY-133152S
-
DM-3411 d8
|
Isotope-Labeled Compounds
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-15780A
-
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 D2L receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole hydrochloride is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM. Brexpiprazole hydrochloride also shows potent antagonist activity at human noradrenergic α1B (Ki=0.17 nM) and α2C receptors (Ki=0.59 nM) .
|
-
- HY-103404
-
-
- HY-17410S
-
-
- HY-18099
-
S1RA
1 Publications Verification
E-52862
|
Sigma Receptor
5-HT Receptor
|
Neurological Disease
|
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
|
-
- HY-B1371A
-
Spiroperidol hydrochloride
|
|
|
Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki 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-HT2A/5-HT1A receptor (Kis 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-14541S
-
LY170053-d3
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
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-105285
-
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-HT1A/5-HT1D agonist, and serotonin 5-HT2B 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
-
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-14541R
-
LY170053 (Standard)
|
5-HT Receptor
Dopamine Receptor
mAChR
Adrenergic Receptor
Autophagy
Mitophagy
Apoptosis
|
Neurological Disease
Cancer
|
Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) 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 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic .
|
-
- HY-106584
-
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-HT 2 receptor. Mosapramine shows antipsychotic activity and can be used in schizophrenia research .
|
-
- HY-101343
-
|
5-HT Receptor
|
Neurological Disease
|
RS 39604 is a potent, selective, and orally active 5-HT4 receptor antagonist with a pKi of 9.1 in guinea pig striatal membranes. RS 39604 displays a low affinity (pKi<6.5) for 5-HT1A, 5-HT2C, 5-HT3, α1c, D1, D2, M1, M2, AT1, B1 and opioid mu receptors and moderate affinity for δ1, (pKi=6.8) and δ2 (pKi=7.8) sites .
|
-
- HY-105542
-
|
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-W050162
-
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 GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A 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-163150
-
|
5-HT Receptor
|
Neurological Disease
|
5-HT6R antagonist 3 (compound 15) is a potent, selective and brain-penetrant 5-HT6R antagonist with Ki values of 14 nM, 3533 nM, 35 nM, 1449 nM for 5-HT6, 5-HT1A, 5-HT2A, 5-HT7, respectively. 5-HT6R antagonist 3 shows anxiolytic-like and properties neuroprotective and procognitive-like effects. 5-HT6R antagonist 3 has the potential for the research of Alzheimer’s Disease .
|
-
- HY-B1396
-
BMY-13754; MJ-13754-1
|
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
Endocrinology
|
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 .
|
-
- HY-103430
-
|
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 (Ki=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
-
|
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 (Ki=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-133112
-
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-136109
-
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-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-14147
-
BRL 24924
|
5-HT Receptor
|
Metabolic Disease
|
Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki 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-B1396S
-
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-B1396S1
-
BMY-13754-d6 dihydrochloride; MJ-13754-1-d6 dihydrochloride
|
Isotope-Labeled Compounds
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-14147A
-
(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 Ki 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-136109B
-
(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-134807
-
|
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 Gq-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-HT1B, 5-HT2B, 5-HT4e, and 5-HT7 .
|
-
- HY-14539
-
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 Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively . Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM) .
|
-
- HY-109067
-
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-109067A
-
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-14539R
-
HF 1854 (Standard)
|
Dopamine Receptor
mAChR
Adrenergic Receptor
5-HT Receptor
|
Neurological Disease
|
Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. 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 Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis 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 |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-14940S
-
|
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 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 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-11018S2
-
|
Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). 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-B1213S
-
|
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 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 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) 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) 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 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 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 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 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) 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 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 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) 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 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) 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 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 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) 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 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 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 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 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 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 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-13575S
-
|
Blonanserin-d8 is a deuterium labeled Blonanserin. Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic[1][2].
|
-
-
- HY-13575S1
-
|
Blonanserin-d5 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 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 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 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 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-B1396S
-
|
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-B1396S1
-
|
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].
|
-
Cat. No. |
Product Name |
Application |
Reactivity |
-
- HY-P83619
-
5-HT-1C; 5-HT-2C; 5-HT1C; 5-HT2C; 5-HTR2C; 5HT1C; 5HT2C; 5HTR2C; 5Hydroxytryptamine 2C receptor; HTr1c; HTR2C
|
WB
|
Human, Mouse, Rat |
Your information is safe with us. * Required Fields.
Inquiry Information
- Product Name:
- Cat. No.:
- Quantity:
- MCE Japan Authorized Agent: