Search Result

Results for "

5-ht5 Receptors Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (59) Adenylate Cyclase (1) Adrenergic Receptor (6) Aryl Hydrocarbon Receptor (1) Autophagy (2) Bacterial (4) CDK (1) Cholinesterase (ChE) (1) Dopamine Receptor (11) Drug Metabolite (3) Endogenous Metabolite (1) FAAH (1) GnRH Receptor (2) iGluR (1) Influenza Virus (1) Isotope-Labeled Compounds (7) mAChR (1) mTOR (2) nAChR (2) P-glycoprotein (7) P2X Receptor (1) Phytohormone (1) Potassium Channel (2) Reference Standards (6) Serotonin Transporter (9) TRP Channel (1)
By Research Areas:	Cancer (9) Cardiovascular Disease (6) Endocrinology (2) Infection (1) Inflammation/Immunology (4) Metabolic Disease (4) Neurological Disease (57)

By Targets:

5-HT Receptor (59)

Adenylate Cyclase (1)

Adrenergic Receptor (6)

Aryl Hydrocarbon Receptor (1)

Autophagy (2)

Bacterial (4)

CDK (1)

Cholinesterase (ChE) (1)

Dopamine Receptor (11)

Drug Metabolite (3)

Endogenous Metabolite (1)

FAAH (1)

GnRH Receptor (2)

iGluR (1)

Influenza Virus (1)

Isotope-Labeled Compounds (7)

mAChR (1)

mTOR (2)

nAChR (2)

P-glycoprotein (7)

P2X Receptor (1)

Phytohormone (1)

Potassium Channel (2)

Reference Standards (6)

Serotonin Transporter (9)

TRP Channel (1)

By Research Areas:

Cancer (9)

Cardiovascular Disease (6)

Endocrinology (2)

Infection (1)

Inflammation/Immunology (4)

Metabolic Disease (4)

Neurological Disease (57)

Inhibitors & Agonists

Screening Libraries

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Serpin

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-15574

Piboserod 3 Publications Verification SB-207266	5-HT Receptor	Cardiovascular Disease
Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a K_i value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure) .

HY-B0352S

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

HY-100943

Cinanserin hydrochloride 1 Publications Verification SQ 10643	5-HT Receptor Influenza Virus	Infection Inflammation/Immunology
Cinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity **5-HT₂ receptor antagonist with a K_i of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT₂** than for the 5-HT₁ receptor (K_i of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro .

HY-105090

Lerisetron	5-HT Receptor	Cardiovascular Disease Neurological Disease
Lerisetron is a potent *5-HT₃* antagonists and possess high-affinity binding for the 5-HT₃ receptors with pK_i value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats .

HY-106807

Litoxetine SL 81.0385	5-HT Receptor	Neurological Disease
Litoxetine (SL 81.0385) is a selective 5-HT uptake inhibitor. Litoxetine is a 5-HT₃ receptor antagonist with a K_i of 85 nM for cerebral 5-HT₃ receptors. Litoxetine is an antidepressant and has antiemetic properties .

HY-168333

5-HT6 inverse agonist 1	5-HT Receptor mTOR CDK	Neurological Disease
5-HT6 inverse agonist 1 (Compound 33) is an antagonist for 5-HT6 receptor with a K_i of 23 nM and a K_b of 6.62 nM. 5-HT6 inverse agonist 1 inhibits the 5-HT6R mediated Cdk5 and mTOR signaling pathway. 5-HT6 inverse agonist 1 reduces tactile hypersensitivity in spinal nerve ligation (SNL)-induced rat model .

HY-159689

Cloroperone	5-HT Receptor	Neurological Disease
Cloroperone is a *5-HT₂* receptor inhibitor with a K_i value of 4.5 nM. Cloroperone can be used in research on psychiatric disorders .

HY-14148

Renzapride hydrochloride	5-HT Receptor	Neurological Disease
Renzapride hydrochloride is a benzamide that inhibits irritable bowel syndrome and has antagonistic activity at 5-HT(3) receptors and agonistic activity at 5-HT(4) receptors. Renzapride hydrochloride also exhibits antagonistic activity at 5-HT(2B) receptors and has a certain affinity for 5-HT(2A) and 5-HT(2C) receptors .

HY-162591

MR33317	Cholinesterase (ChE) 5-HT Receptor	Neurological Disease
MR33317 is an inhibitor of acetylcholinesterase with an IC₅₀ value of 41nM. MR33317 is also an agonist at brain *5-HT₄ receptors* .

HY-103114

AT1015 hydrochloride	5-HT Receptor	Cardiovascular Disease Neurological Disease
AT1015 hydrochloride is a potent antagonist of **5-HT₂ receptor, with the pK_i** of 7.94. AT1015 inhibits vasoconstriction and blocks platelet aggregation .

HY-19927A

DA-6886 monohydrochloride	5-HT Receptor	Neurological Disease Endocrinology
DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a *5-HT4* receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC₅₀ value of 4.3, indicating that the compound is 1000-fold more selective for the *5-HT4* receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome .

HY-105090R

Lerisetron (Standard)	5-HT Receptor	Cardiovascular Disease Neurological Disease Cancer
Lerisetron (Standard) is the analytical standard of Lerisetron. This product is intended for research and analytical applications. Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats .

HY-11018

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

HY-138176

7-Hydroxyrisperidone 7-RispOH	Drug Metabolite	Neurological Disease
7-Hydroxyrisperidone (7-RispOH) is a metabolite of Risperidone (HY-11018). Risperidone is a serotonin 5-HT₂ receptor blocker, P-Glycoprotein inhibitor and potent dopamine D₂ receptor antagonist .

HY-11018A

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

HY-168537

LB-102	Dopamine Receptor 5-HT Receptor	Neurological Disease
LB-102 is an orally active inhibitor of dopamine D₂, D₃, and *5-HT7* receptors, which can be used in research on schizophrenia and other psychiatric disorders .

HY-118775

LEK 8804	5-HT Receptor	Others
LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.

HY-11018B

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

HY-B0020

Tropisetron Hydrochloride 4 Publications Verification SDZ-ICS-930	5-HT Receptor nAChR	Neurological Disease Inflammation/Immunology Cancer
Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a *5-HT3* receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC₅₀ of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation .

HY-100552

VUF10166	5-HT Receptor	Neurological Disease
VUF10166 is a potent and high-affinity **5-HT₃ receptor antagonist, with K_i** values of 0.04 nM (5-HT₃A) and 22 nM (5-HT₃AB). VUF10166 inhibits 5-HT-induced responses at 5-HT₃A and 5-HT₃AB receptors at nanomolar concentrations. At **5-HT₃ receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC₅₀** of 5.2 μM .

HY-123206

R-96544 free base	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-110232

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

HY-121704

SR 57227A free base	iGluR	Neurological Disease
SR 57227A Free base is a highly selective compound for both peripheral and central 5-HT3 receptors and acts as an inhibitor of NMDA receptor-mediated responses in rat cortical pyramidal cells, demonstrating antidepressant-like effects in rats while reducing isolation-induced aggressive behavior.

HY-B0020R

Tropisetron (Hydrochloride) (Standard) SDZ-ICS-9323 (Standard)	5-HT Receptor nAChR	Neurological Disease Cancer
Tropisetron (Hydrochloride) (Standard) is the analytical standard of Tropisetron (Hydrochloride). Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a *5-HT3* receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC₅₀ of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation .

HY-135194

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

HY-11018R

Risperidone (Standard) R 64 766 (Standard)	Dopamine Receptor 5-HT Receptor P-glycoprotein Reference Standards	Neurological Disease
Risperidone (Standard) is the analytical standard of Risperidone. This product is intended for research and analytical applications. Risperidone is a serotonin **5-HT₂ receptor blocker, P-Glycoprotein** inhibitor and potent dopamine D₂ receptor antagonist, with K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-101172

RS 23597-190 EP-A-501322	5-HT Receptor	Cardiovascular Disease
RS 23597-190 (EP-A-501322) is a high affinity and selective 5-HT4 receptor antagonist. RS 23597-190 inhibits 5-HT-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .

HY-19136

WAY-100289	5-HT Receptor	Neurological Disease
WAY-100289 is an orally active antagonist for 5-HT3 receptor, that exhibits high affinity to the isolated rat vagus nerves with pA₂ of 8.9. WAY-100289 inhibits the Bezold-Jarisch reflex in anesthetized and awake rats .

HY-117046

AVN-101	5-HT Receptor	Neurological Disease
AVN-101 free base is a multi-target drug candidate with the potential to inhibit central nervous system (CNS) diseases. AVN-101 free base exhibits high inhibitory activity on 5-HT7 receptors and also has certain activity on 5-HT6, 5-HT2A and 5-HT2C receptors. Due to its anxiolytic and antidepressant activities, AVN-101 free base is also expected to be used in diseases such as general anxiety disorder, depression, schizophrenia and multiple sclerosis .

HY-106407

Beloxepin Org 4428; ADL 6906	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Beloxepin (Org 4428) is an orally active synaptosomal noradrenalin reuptake inhibitor and a 5-HT2 receptor antagonist. Beloxepin shows about 100-fold less affine for other monoamine carriers. Beloxepin has antidepressant and pain-relieving effects .

HY-11018S1

Risperidone-d4-1 R 64 766-d₄-1	Isotope-Labeled Compounds Dopamine Receptor P-glycoprotein 5-HT Receptor	Neurological Disease
Risperidone-d4-1 (R 64 766-d4-1) 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 K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-11018S2

Risperidone-d6 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 K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively .

HY-123044

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

HY-32329

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

HY-135194R

Risperidone E-oxime (Standard)	Drug Metabolite Reference Standards	Others
Risperidone E-oxime (Standard) is the analytical standard of Risperidone E-oxime. This product is intended for research and analytical applications. 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-14149A

Cisapride monohydrate R 51619 monohydrate; (±)-Cisaprid monohydrate	5-HT Receptor	Neurological Disease Metabolic Disease
Cisapride monohydrate is an orally and potent *5-HT₄* receptor agonist and hERG inhibitor. Cisapride monohydrate is an prokinetic agent which facilitates or restores motility throughout the length of the gastrointestinal tract. Cisapride monohydrate stimulates gastrointestinal motor activity through an indirect mechanism involving the release of acetylcholine mediated by postganglionic nerve endings in the myenteric plexus of the gut .

HY-101755

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

HY-32329A

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

HY-134807

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

HY-103337

N-Arachidonoylserotonin Arachidonyl serotonin; AA-5-ht	FAAH TRP Channel	Neurological Disease
N-Arachidonoylserotonin (Arachidonyl serotonin; AA-5-HT) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC₅₀ value of 1~12 µM. N-Arachidonoylserotonin acts also as an antagonist of transient receptor potential vanilloid-type 1 (TRPV1) channels (IC₅₀=70~100 nM). N-Arachidonoylserotonin is analgesic in rodents .

HY-120464

PF-05212377 SAM-760	5-HT Receptor	Neurological Disease
PF-05212377 (SAM-760) is an inhibitor for serotonin receptor 5-HT6. PF-05212377 is a substrate for P-gp/non-BCRP human transporter. PF-05212377 exhibits blood brain barrier permeability in non-human primates. PF-05212377 can be used for Alzheimer’s Disease research .

HY-15414

Vortioxetine 5+ Cited Publications Lu AA 21004	5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial agonist of 5-HT_1B (K_i: 15 nM, 33 nM) .

HY-B2065

Scopolamine hydrochloride (-)-Scopolamine hydrochloride; Hyoscine hydrochloride	mAChR 5-HT Receptor	Neurological Disease
Scopolamine hydrochloride is a non-selective and high affinity (≤1 nM) muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. Scopolamine readily passes the blood brain barrier. Scopolamine also reversibly inhibits *5-HT3* receptor-responses with an IC₅₀ of 2.09 μM . Scopolamine induces Alzheimer's disease-like pathology through alteration of cholinergic system .

HY-121311

Metrenperone	Serotonin Transporter Adrenergic Receptor	Cardiovascular Disease
Metrenperone is an inhibitor for 5-HT2 receptor. Metrenperone exhibits α1 and α2 antagonist activity as well as anti-H1 and anti-dopaminergic efficacy. Metrenperone can lower the blood pressure, enhances bradycardia in peripheral ischemia, inhibits serotonin-induced platelet aggregation, and antagonizes serotonin-mediated vasoconstriction. Metrenperone promotes the repair of acutely damaged collagen tissue .

HY-32329S

Setiptiline-d3	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 .

HY-P3641

Kisspeptin 13	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

HY-121562

SB 714786	5-HT Receptor	Neurological Disease
SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.

HY-15414A

Vortioxetine hydrobromide 5+ Cited Publications Lu AA21004 hydrobromide	5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-106379

Lurosetron GR-87442	5-HT Receptor	Neurological Disease
Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron (HY-70050A). Lurosetron is a serotonin 5-HT3 receptor antagonist. Lurosetron inhibits recombinant (rbt) CYP1A2, with an IC₅₀ of 0.1 μM. Lurosetron also inhibits other CYP isoforms, including rbtCYP2C9 and rbtCYP3A4 with IC₅₀s ranging between 3.5 μM and 16 μM. .

HY-172678

PUC-10	5-HT Receptor mTOR Autophagy	Neurological Disease
PUC-10 is a **5-HT₆ receptor antagonist with a K_i of 14.6 nM and an IC₅₀** of 32 nM. In silico predictions suggest that PUC-10 is orally active and can cross the blood-brain barrier. PUC-10 can induce autophagy in SH-SY5Y cells by inhibiting the mTOR pathway. PUC-10 can be used in the research of neurological disorders .

Cat. No.	Product Name

HY-L121

5-HT Receptor Compound Library

356 compounds

5-HT receptors, also called Serotonin receptors, are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. These receptors are now classified into seven families, 5-HT1–7, comprising a total of 14 structurally and pharmacologically distinct mammalian 5-HT receptor subtypes. The 5-HT receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics, antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.

MCE 5-HT Receptor Compound Library consists of 356 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

Cat. No.	Product Name	Target	Research Area

HY-P3641A

Kisspeptin 13 TFA	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

HY-P3641

Kisspeptin 13	GnRH Receptor	Neurological Disease Metabolic Disease
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC₅₀ of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Alkaloids Structural Classification Microorganisms Classification of Application Fields Other Diseases Endogenous metabolite Disease Research Fields Indole Alkaloids	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor
Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models .

HY-B2065

Scopolamine hydrochloride (-)-Scopolamine hydrochloride; Hyoscine hydrochloride	Alkaloids Structural Classification Other Alkaloids Source classification Atropa belladonna Linn. Solanaceae Plants	mAChR 5-HT Receptor
Scopolamine hydrochloride is a non-selective and high affinity (≤1 nM) muscarinic antagonist that is used for the prevention of post-operative nausea and vomiting. Scopolamine readily passes the blood brain barrier. Scopolamine also reversibly inhibits *5-HT3* receptor-responses with an IC₅₀ of 2.09 μM . Scopolamine induces Alzheimer's disease-like pathology through alteration of cholinergic system .

HY-N9418R

Gibberellin A5 (Standard)	Source classification Rosaceae Plants Rosa canina Gremli ex Christ	Phytohormone Reference Standards
Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. 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 .

Cat. No.	Product Name	Chemical Structure

HY-B0352S

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

HY-110232

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

HY-11018S1

Risperidone-d4-1
Risperidone-d4-1 (R 64 766-d4-1) 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 K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively.

HY-11018S2

Risperidone-d6
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 K_is of 4.8, 5.9 nM for 5-HT_2A and dopamine D₂ receptor, respectively .

HY-32329S

Setiptiline-d3

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

HY-15414S

Vortioxetine-d8
Vortioxetine-d₈ (Lu AA 21004-d₈) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-15414S2

Vortioxetine-d4
Vortioxetine-d₄ (Lu AA 21004-d₄) is the deuterium labeled Vortioxetine (HY-15414). Vortioxetine is an antagonist of 5-HT3A and 5-HT7 receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT1A agonist and a partial agonist of 5-HT1B (K_i: 15 nM, 33 nM) .

HY-15414AS

Vortioxetine-d8 hydrobromide
Vortioxetine-d₈ (Lu AA 21004-d₈) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

HY-15414S3

Vortioxetine-d3
Vortioxetine-d₃ (Lu AA 21004-d₃) is a deuterium labeled Vortioxetine (HY-15414). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial agonist of 5-HT_1B (K_i: 15 nM, 33 nM) .

HY-15414S1

Vortioxetine-d6
Vortioxetine-d6 (Lu AA 21004-d6) is the deuterium labeled Vortioxetine (HY-B1490A). Vortioxetine (Lu AA 21004) is an antagonist of 5-HT_3A and 5-HT₇ receptors (K_i: 3.7 nM, 19 nM) and an inhibitor of serotonin transporter (SERT) (K_i: 1.6 nM), as well as a 5-HT_1A agonist and a partial agonist of 5-HT_1B (K_i: 15 nM, 33 nM) .

Inquiry Online

Your information is safe with us. * Required Fields.

MCE Japan Authorized Agent ナミキ商事株式会社コスモ・バイオ株式会社
Salutation			Country or Region *
Applicant Name *			Organization Name *
Department *
Email Address *			Product Name *
Cat. No.			Requested quantity *
Phone Number *
Remarks