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5-ht5 Receptors Inhibitors

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (109) Adenylate Cyclase (3) Adrenergic Receptor (11) Akt (1) Apoptosis (2) Aryl Hydrocarbon Receptor (1) Autophagy (2) Bacterial (6) Biochemical Assay Reagents (1) CDK (1) Cholinesterase (ChE) (1) Cytochrome P450 (1) DNA/RNA Synthesis (2) Dopamine Receptor (17) Dopamine Transporter (1) Drug Metabolite (5) Endogenous Metabolite (1) Epigenetic Reader Domain (2) ERK (2) FAAH (2) GABA Receptor (1) GnRH Receptor (2) HCN Channel (2) Histamine Receptor (5) iGluR (1) Influenza Virus (2) Isotope-Labeled Compounds (14) mAChR (3) MMP (2) Monoamine Transporter (1) mTOR (2) nAChR (4) P-glycoprotein (7) P2X Receptor (1) Phytohormone (1) Potassium Channel (3) Reactive Oxygen Species (ROS) (2) Reference Standards (21) Serotonin Transporter (15) Sigma Receptor (1) TRP Channel (1)
By Research Areas:	Cancer (16) Cardiovascular Disease (12) Endocrinology (3) Infection (3) Inflammation/Immunology (11) Metabolic Disease (7) Neurological Disease (94)

By Targets:

5-HT Receptor (109)

Adenylate Cyclase (3)

Adrenergic Receptor (11)

Akt (1)

Apoptosis (2)

Aryl Hydrocarbon Receptor (1)

Autophagy (2)

Bacterial (6)

Biochemical Assay Reagents (1)

CDK (1)

Cholinesterase (ChE) (1)

Cytochrome P450 (1)

DNA/RNA Synthesis (2)

Dopamine Receptor (17)

Dopamine Transporter (1)

Drug Metabolite (5)

Endogenous Metabolite (1)

Epigenetic Reader Domain (2)

ERK (2)

FAAH (2)

GABA Receptor (1)

GnRH Receptor (2)

HCN Channel (2)

Histamine Receptor (5)

iGluR (1)

Influenza Virus (2)

Isotope-Labeled Compounds (14)

mAChR (3)

MMP (2)

Monoamine Transporter (1)

mTOR (2)

nAChR (4)

P-glycoprotein (7)

P2X Receptor (1)

Phytohormone (1)

Potassium Channel (3)

Reactive Oxygen Species (ROS) (2)

Reference Standards (21)

Serotonin Transporter (15)

Sigma Receptor (1)

TRP Channel (1)

By Research Areas:

Cancer (16)

Cardiovascular Disease (12)

Endocrinology (3)

Infection (3)

Inflammation/Immunology (11)

Metabolic Disease (7)

Neurological Disease (94)

119

Inhibitors & Agonists

Bibliotecas de Screening

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Serpin

Cat. No.	Nombre del producto	Target	Áreas de investigación	Chemical Structure

HY-19545A

SCH-23390 hydrochloride Maximum Cited Publications 31 Publications Verification R-(+)-SCH-23390 hydrochloride	Dopamine Receptor 5-HT Receptor Potassium Channel	Neurological Disease
SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D₁-like receptor antagonist with K_is of 0.2 nM and 0.3 nM for the D₁ and D₅ receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT_2C receptor agonist with a K_i of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the *5-HT₂* and 5-HT_1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC₅₀ of 268 nM .

HY-11018

Risperidone 5+ Cited Publications 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-B0002B

Ondansetron 5+ Cited Publications GR 38032; SN 307	5-HT Receptor	Neurological Disease
Ondansetron (GR 38032; SN 307) is a highly selective *5-HT₃* receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Endogenous Metabolite 5-HT Receptor Aryl Hydrocarbon Receptor	Neurological Disease Metabolic Disease
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-15414

Vortioxetine 5+ Cited Publications Lu AA 21004	5-HT Receptor Serotonin Transporter	Infection 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-B0002

Ondansetron hydrochloride 5+ Cited Publications GR 38032 hydrochloride; SN 307 hydrochloride	5-HT Receptor	Neurological Disease
Ondansetron (GR 38032; SN 307) hydrochloride is a highly selective *5-HT₃* receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron hydrochloride exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .

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-B0002A

Ondansetron hydrochloride dihydrate 5+ Cited Publications GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrate	5-HT Receptor	Neurological Disease
Ondansetron (GR 38032; SN 307) hydrochloride dehydrate is a highly selective *5-HT₃* receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron hydrochloride dehydrate exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride dehydrate can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .

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-B1107

Naftidrofuryl oxalate Nafronyl oxalate salt	5-HT Receptor	Cardiovascular Disease
Naftidrofuryl oxalate (Nafronyl oxalate salt) is an orally active 5-HT₂ receptor antagonist. Naftidrofuryl oxalate selectively blocks vascular and platelet 5-HT₂ receptors, inhibiting Serotonin (HY-B1473A)-induced vasoconstriction, platelet aggregation, and vascular smooth muscle cell proliferation. Naftidrofuryl oxalate can be used for the research of intermittent claudication, peripheral occlusive arterial disease, and critical limb ischaemia .

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-B0383

Almotriptan malate PNU180638	5-HT Receptor	Neurological Disease
Almotriptan malate (PNU180638) is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine .

HY-15574

Piboserod 4 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-75813

2-Aminonicotinaldehyde	Biochemical Assay Reagents Akt 5-HT Receptor	Neurological Disease Cancer
2-Aminonicotinaldehyde is a synthetic intermediate. 2-Aminonicotinaldehyde can be used for the synthesis of *5-HT3* receptor antagonists, AKT inhibitors, and other compounds. 2-Aminonicotinaldehyde is applicable to research on depression and cancers (including hepatocellular carcinoma) .

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-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 Serotonin (HY-B1473A)-induced tachycardia. RS 23597-190 significantly inhibits superoxide production in high glucose .

HY-B0383A

Almotriptan PNU180638 free base	5-HT Receptor	Neurological Disease
Almotriptan (PNU180638 free base) is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan can be used in research related to migraine .

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-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-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-A0075

Decloxizine dihydrochloride 1 Publications Verification UCB 1402 dihydrochloride; NSC289116 dihydrochloride	Histamine Receptor 5-HT Receptor	Inflammation/Immunology
Decloxizine (UCB-1402; NSC289116) dihydrochloride is an orally active bronchodilator that can penetrate the blood-brain barrier. Decloxizine dihydrochloride is a piperazine-type H₁ histamine receptor antagonist. Decloxizine dihydrochloride selectively blocks H1 histamine receptors, inhibiting histamine-induced capillary dilation, edema, and itching. Decloxizine dihydrochloride has some **5-HT₂ receptor** antagonistic activity. Decloxizine dihydrochloride can be used in studies of urticaria, allergic rhinitis, and bronchial asthma .

HY-15414R

Vortioxetine (Standard) Lu AA 21004 (Standard)	Reference Standards 5-HT Receptor Serotonin Transporter	Neurological Disease Cancer
Vortioxetine (Standard) is an analytical standard for Vortioxetine. This product is intended for research and analytical applications. 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 5-HT_1B agonist (K_i: 15 nM, 33 nM) .

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-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-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-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-N4157

Isopteropodine	mAChR 5-HT Receptor Bacterial	Neurological Disease
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial** activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-B0002BS

Ondansetron-d5 GR 38032-d₅; SN 307-d₅	5-HT Receptor Isotope-Labeled Compounds	Neurological Disease
Ondansetron-d₅ is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective *5-HT₃* receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .

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-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-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-135439

SB-203186	5-HT Receptor	Neurological Disease
SB-203186 is a highly selective 5-HT₄ receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pK_B value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .

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-175816

5-HT6R/FAAH modulator 1	5-HT Receptor FAAH Apoptosis Reactive Oxygen Species (ROS)	Neurological Disease
5-HT6R/FAAH modulator 1 is a selective serotonin 5-HT6 receptor ligand and the fatty acid amide hydrolase (FAAH) enzyme inhibitor. 5-HT6R/FAAH modulator 1 shows a pK_i of 6.33 (5-HT6) and a pIC₅₀ valuesof 6.29 (FAAH). 5-HT6R/FAAH modulator 1 also slightly inhibits acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) enzymes (pIC₅₀ = 5.12). 5-HT6R/FAAH modulator 1 can inhibit apoptosis and reduce ROS levels. 5-HT6R/FAAH modulator 1 can be used for the research of neurological disease, such as Alzheimer’s disease (AD) .

HY-15414AR

Vortioxetine hydrobromide (Standard) Lu AA21004 hydrobromide (Standard)	5-HT Receptor Serotonin Transporter Reference Standards	Neurological Disease Cancer
Vortioxetine (hydrobromide) (Standard) is the analytical standard of Vortioxetine (hydrobromide). This product is intended for research and analytical applications. Vortioxetine (Lu AA 21004) hydrobromide is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM) .

HY-15414S

Vortioxetine-d8 Lu AA 21004 d₈	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease
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-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-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-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-17582

Decloxizine 1 Publications Verification UCB-1402; NSC289116	Histamine Receptor 5-HT Receptor	Inflammation/Immunology
Decloxizine (UCB-1402; NSC289116) is an orally active bronchodilator that can penetrate the blood-brain barrier. Decloxizine is a piperazine-type H₁ histamine receptor antagonist. Decloxizine selectively blocks H1 histamine receptors, inhibiting histamine-induced capillary dilation, edema, and itching. Decloxizine has some **5-HT₂ receptor** antagonistic activity. Decloxizine can be used in studies of urticaria, allergic rhinitis, and bronchial asthma .

HY-14149A

Cisapride monohydrate 2 Publications Verification 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-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-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-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-108400

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

HY-W052508R

Norquetiapine (Standard) N-Desalkylquetiapine (Standard)	5-HT Receptor Reference Standards	Neurological Disease
Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .

HY-15414AS

Vortioxetine-d8 hydrobromide Lu AA21004-d8 hydrobromide	Isotope-Labeled Compounds 5-HT Receptor Serotonin Transporter	Neurological Disease
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-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 .

Cat. No.	Nombre del producto

HY-L121

5-HT Receptor Compound Library

414 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 414 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

Cat. No.	Nombre del producto	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.	Nombre del producto	Category	Target	Chemical Structure

HY-B2132

Tryptamine 1 Publications Verification 3-(2-Aminoethyl)indole~2-(3-Indolyl)ethylamine	Alkaloids 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-N4157

Isopteropodine	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	mAChR 5-HT Receptor Bacterial
Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial** activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-N4157R

Isopteropodine (Standard)	Uncaria rhynchophylla (Miq.) Miq. ex Havil. Structural Classification Iridoids Terpenoids Rubiaceae Plants Source Classification	Reference Standards mAChR 5-HT Receptor Bacterial
Isopteropodine (Standard) is the analytical standard of Isopteropodine (HY-N4157). This product is intended for research and analytical applications. Isopteropodine is a positive modulator that selectively acts on muscarinic M₁ and **5-HT₂ receptors. Isopteropodine has an EC₅₀ of 9.92 μM for acetylcholine and 14.5 μM for 5-HT. Isopteropodine also has antibacterial** activity against Gram-positive bacteria, with MICs of 150 μg/mL and 250 μg/mL for Staphylococcus aureus and Bacillus subtilis, respectively. Isopteropodine enhances receptor function by increasing the affinity of agonists for receptors and can also inhibit the growth of specific Gram-positive bacteria, and can be used in cognitive impairment and antibacterial research .

HY-N9418R

Gibberellin A5 (Standard)	Rosaceae Plants Rosa canina Gremli ex Christ Source Classification	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.	Nombre del producto	Chemical Structure

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-B0002BS

Ondansetron-d5

Ondansetron-d₅ is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT₃ receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .

HY-W052508S

Norquetiapine-d8

Norquetiapine-d8 (N-Desalkylquetiapine-d8) is the deuterium labeled Norquetiapine.Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC₅₀ of 13.9 μM. Norquetiapine selectively inhibits noradrenaline reuptake, is a partial 5-HT_1A (K_i = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (K_i = 237 nM), 5-HT_2C(K_i = 107 nM), and 5-HT₇ (K_i = 76 nM) receptors. Norquetiapine blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation .

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-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-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-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-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-B0383AS

Almotriptan hydrochloride-d6

Almotriptan-d₆ (PNU180638-d₆) hydrochloride is the deuterium labeled Almotriptan hydrochloride. Almotriptan hydrochloride is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan hydrochloride shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan hydrochloride induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan hydrochloride can be used in research related to migraine.

HY-B0383AS2

Almotriptan-d3 benzoate

Almotriptan-d₃ benzoate (PNU180638 free base-d₃) is deuterated labeled Almotriptan benzoate. Almotriptan benzoate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan benzoate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan benzoate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan benzoate can be used in research related to migraine.

HY-143797S

Almotriptan-d6 maleate

Almotriptan-d₆ (PNU180638-d₆) maleate is the deuterium labeled Almotriptan maleate. Almotriptan malate is an orally active, highly selective agonist of the 5-HT_1B/1D receptor (5-HT_1B/1D receptor), with EC₅₀ values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.

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-B0002BS1

Ondansetron-d3

Ondansetron-d₃ is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT₃ receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .

HY-B0002BS2

Ondansetron-13C,d3

Ondansetron- ¹³C,d₃ is the ¹³C- and deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT₃ receptor antagonist with an IC₅₀ value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy .

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-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) .

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