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5-HT Receptor Antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (703) Adenylate Cyclase (5) Adrenergic Receptor (119) Akt (3) AP-1 (1) Apoptosis (20) Arrestin (1) Autophagy (17) Bacterial (7) Biochemical Assay Reagents (3) Calcium Channel (3) Cannabinoid Receptor (1) Caspase (2) CDK (1) CGRP Receptor (1) Chloride Channel (1) COMT (1) COX (2) Cytochrome P450 (4) Dopamine Receptor (217) Dopamine Transporter (1) Drug Derivative (1) Drug Isomer (1) Drug Metabolite (20) Endogenous Metabolite (7) Epigenetic Reader Domain (2) ERK (1) FAAH (1) FGFR (2) FOXO (1) G protein-coupled Bile Acid Receptor 1 (2) G Protein-coupled Receptor Kinase (GRK) (1) GABA Receptor (1) Glycine Receptor (GlyR) (1) GlyT (3) HCN Channel (2) HCV Protease (1) Histamine Receptor (31) iGluR (1) Influenza Virus (2) Isotope-Labeled Compounds (79) JAK (1) Ligands for E3 Ligase (1) mAChR (18) MDM-2/p53 (1) Melatonin Receptor (11) Mitophagy (5) Monoamine Oxidase (1) mTOR (2) nAChR (12) NF-κB (1) Nuclear Factor of activated T Cells (NFAT) (1) Opioid Receptor (1) Orexin Receptor (OX Receptor) (3) P-glycoprotein (7) P2X Receptor (6) p38 MAPK (3) Parasite (5) Phosphatase (1) Phosphodiesterase (PDE) (1) Phytohormone (1) PKC (4) Potassium Channel (7) Reactive Oxygen Species (ROS) (3) Reference Standards (121) Renin (3) Ribosomal S6 Kinase (RSK) (1) RSV (1) Serotonin Transporter (18) Sigma Receptor (10) Sodium Channel (4) TGF-β Receptor (2) Transthyretin (TTR) (2) TRP Channel (3) Wnt (2)
By Research Areas:	Cancer (86) Cardiovascular Disease (68) Endocrinology (45) Infection (17) Inflammation/Immunology (48) Metabolic Disease (37) Neurological Disease (631)

By Targets:

5-HT Receptor (703)

Adenylate Cyclase (5)

Adrenergic Receptor (119)

Akt (3)

AP-1 (1)

Apoptosis (20)

Arrestin (1)

Autophagy (17)

Bacterial (7)

Biochemical Assay Reagents (3)

Calcium Channel (3)

Cannabinoid Receptor (1)

Caspase (2)

CDK (1)

CGRP Receptor (1)

Chloride Channel (1)

COMT (1)

COX (2)

Cytochrome P450 (4)

Dopamine Receptor (217)

Dopamine Transporter (1)

Drug Derivative (1)

Drug Isomer (1)

Drug Metabolite (20)

Endogenous Metabolite (7)

Epigenetic Reader Domain (2)

ERK (1)

FAAH (1)

FGFR (2)

FOXO (1)

G protein-coupled Bile Acid Receptor 1 (2)

G Protein-coupled Receptor Kinase (GRK) (1)

GABA Receptor (1)

Glycine Receptor (GlyR) (1)

GlyT (3)

HCN Channel (2)

HCV Protease (1)

Histamine Receptor (31)

iGluR (1)

Influenza Virus (2)

Isotope-Labeled Compounds (79)

JAK (1)

Ligands for E3 Ligase (1)

mAChR (18)

MDM-2/p53 (1)

Melatonin Receptor (11)

Mitophagy (5)

Monoamine Oxidase (1)

mTOR (2)

nAChR (12)

NF-κB (1)

Nuclear Factor of activated T Cells (NFAT) (1)

Opioid Receptor (1)

Orexin Receptor (OX Receptor) (3)

P-glycoprotein (7)

P2X Receptor (6)

p38 MAPK (3)

Parasite (5)

Phosphatase (1)

Phosphodiesterase (PDE) (1)

Phytohormone (1)

PKC (4)

Potassium Channel (7)

Reactive Oxygen Species (ROS) (3)

Reference Standards (121)

Renin (3)

Ribosomal S6 Kinase (RSK) (1)

RSV (1)

Serotonin Transporter (18)

Sigma Receptor (10)

Sodium Channel (4)

TGF-β Receptor (2)

Transthyretin (TTR) (2)

TRP Channel (3)

Wnt (2)

By Research Areas:

Cancer (86)

Cardiovascular Disease (68)

Endocrinology (45)

Infection (17)

Inflammation/Immunology (48)

Metabolic Disease (37)

Neurological Disease (631)

758

Inhibitors & Agonists

Biochemical Assay Reagents

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: 5-HT Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-14544

Quetiapine 3 Publications Verification ICI204636	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine (ICI204636) is a **5-HT receptors agonist with a pEC₅₀** of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, *5-HT2A, *5-HT2C receptor with pK_i**s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-B0982

Pindolol 2 Publications Verification LB-46	5-HT Receptor Adrenergic Receptor	Neurological Disease
Pindolol (LB-46) is the antagonist for 5-HT 1A (K_i=33 nM) and 5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor. Pindolol exhibits anti-anxiety and antidepressant effects .

HY-15370A

SB-269970 hydrochloride 5+ Cited Publications SB-269970A	5-HT Receptor	Neurological Disease
SB-269970 hydrochloride is a potent, selective and brain-penetrant **5-HT7 receptor** antagonist with a pK_i of 8.3. SB-269970 hydrochloride exhibits >50-fold selectivity against other 5-HT receptors .

HY-B1033

Metergoline 2 Publications Verification	5-HT Receptor Dopamine Receptor Sodium Channel	Neurological Disease
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pK_is of 8.64, 8.75 and 8.75 for 5-HT_2A, 5-HT_2B and 5-HT_2C, respectively. Metergoline is a high-affinity ligand for the h5-HT₇ receptor, with a K_i of 16 nM. Metergoline is also a reversible neural Na ⁺ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .

HY-14542

Ziprasidone 3 Publications Verification CP-88059	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059), an orally active antipsychotic agent, is a combined *5-HT* and dopamine receptor antagonist . Ziprasidone mesylate trihydrate has affinities for Rat D₂ (K_i=4.8 nM), *5-HT_2A* (K_i=0.42 nM) and *5-HT_1A* (K_i=3.4 nM) .

HY-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-17407

Ziprasidone hydrochloride monohydrate 3 Publications Verification CP 88059 hydrochloride monohydrate	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined *5-HT* and dopamine receptor antagonist . Ziprasidone hydrochloride monohydrate has affinities for Rat D₂ (K_i=4.8 nM), *5-HT_2A* (K_i=0.42 nM) and *5-HT_1A* (K_i=3.4 nM) .

HY-B0031

Quetiapine hemifumarate 3 Publications Verification	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine hemifumarate is a **5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor*. Quetiapine hemifumarate is a dopamine receptor* antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, *5-HT2A, *5-HT2C receptor with pK_i**s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-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-B1154

Penbutolol sulfate 1 Publications Verification (-)-Terbuclomine	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Penbutolol sulfate ((-)-Terbuclomine) is a potent β-adrenoceptor and 5-HT receptor antagonist with K_i of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 .

HY-14542A

Ziprasidone hydrochloride 3 Publications Verification CP-88059 hydrochloride	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone (CP-88059) hydrochloride is an orally active combined *5-HT* and dopamine receptor antagonist . Ziprasidone hydrochloride has affinities for Rat D₂ (K_i=4.8 nM), *5-HT_2A* (K_i=0.42 nM) and *5-HT_1A* (K_i=3.4 nM) .

HY-17390A

Loxapine succinate 1 Publications Verification	5-HT Receptor Dopamine Receptor	Infection Neurological Disease
Loxapine succinate is an orally active dopamine inhibitor, **5-HT receptor** antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages .

HY-17390

Loxapine 1 Publications Verification	5-HT Receptor Dopamine Receptor Bacterial	Neurological Disease
Loxapine is an orally active dopamine inhibitor, **5-HT receptor** antagonist and also a dibenzoxazepine anti-psychotic agent .

HY-100562

Flopropione	5-HT Receptor COMT	Neurological Disease
Flopropione is a **5-HT receptor** antagonist and also a catechol-o-methyltransferase (COMT) inhibitor . Flopropione also as an antispasmodic agent .

HY-15370

SB-269970 5+ Cited Publications	5-HT Receptor	Neurological Disease
SB-269970 is a potent, selective and brain-penetrant **5-HT7 receptor** antagonist with a pK_i of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors .

HY-109112

Brilaroxazine 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 (K_i=1.5 nM) and 5-HT2A (K_i=2.5 nM), and has antagonist activity at 5-HT2B (K_i=0.19 nM), and 5-HT7 (K_i=2.7 nM) receptors . Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo .

HY-19818A

NAN-190 hydrobromide	5-HT Receptor	Neurological Disease
NAN-190 hydrobromide is a serotonin receptor *5-HT* antagonist. NAN-190 is a selective antagonist of *5-HT_1A* .

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-G0014A

Quetiapine sulfoxide dihydrochloride 1 Publications Verification Quetiapine S-oxide dihydrochloride	Drug Metabolite	Neurological Disease
Quetiapine sulfoxide dihydrochloride (Quetiapine S-oxide dihydrochloride) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic . Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist .

HY-103156

NAS-181 dimesylate 3 Publications Verification	5-HT Receptor	Neurological Disease
NAS181 is a potent and selective antagonist of rat 5-HT_1B receptor, with a K_i of 47 nM. NAS181 shows 13-fold selectivity for r5-HT_1B over bovine 5-HT_1B receptor (K_i=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT_1B autoreceptors .

HY-131255

Ziprasidone amino acid Ziprasidone Impurity C; Ziprasidone open ring impurity	5-HT Receptor Dopamine Receptor	Neurological Disease
Ziprasidone amino acid (Ziprasidone Impurity C) is an impurity of Ziprasidone. Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone exhibits potent effects of antipsychotic activity .

HY-116790

(-)-Penbutolol 1 Publications Verification (S)-Penbutolol; (-)-Isopenbutolol	Adrenergic Receptor 5-HT Receptor	Neurological Disease
(-)-Penbutolol ((S)-Penbutolol) is a potent β-adrenoceptor and **5-HT receptor** antagonist with K_i values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 .

HY-100851A

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

HY-14544R

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

HY-101222

SB-203186 hydrochloride	5-HT Receptor	Cardiovascular Disease Neurological Disease
SB-203186 hydrochloride is a potent, selective and competitive *5-HT₄* antagonist. SB-203186 hydrochloride antagonizes the 5-HT₄ receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pK_B values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively .

HY-B0031R

Quetiapine hemifumarate (Standard)	Reference Standards 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 pK_i**s of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-B0031S1

Quetiapine-d4 hemifumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine-d₄ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .

HY-B0982R

Pindolol (Standard) LB-46 (Standard)	Reference Standards 5-HT Receptor Adrenergic Receptor	Neurological Disease
Pindolol (Standard) is the analytical standard of Pindolol. This product is intended for research and analytical applications. Pindolol (LB-46) is the antagonist for 5-HT 1A (K_i=33 nM) and 5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor. Pindolol exhibits anti-anxiety and antidepressant effects .

HY-W016194

1-(Carboxymethyl)cyclohexanecarboxylic acid 1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E; Gabapentin Related Compound E	5-HT Receptor	Neurological Disease
1-(Carboxymethyl)cyclohexanecarboxylic acid (1-Carboxycyclohexaneacetic acid; Gabapentin Impurity E) is a potential impurity in commercial preparations of the antiepileptic agent Gabapentin (HY-A0057). It is also used as a precursor for the synthesis of a serotonin (5-HT) receptor subtype 5-HT2A antagonist.

HY-101480

Xylamidine	5-HT Receptor	Neurological Disease
Xylamidine is a peripheral 5-HT receptor antagonist used to investigate possible peripheral appetite suppressant effects of 5-hydroxytryptophan (5-HTP) and fenfluramine. In a 1-hour food intake test, xylamidine attenuated the decrease in food intake induced by 5-HT and 5-HTP, but had no effect on fenfluramine, suggesting that the appetite suppressant effect of 5-HTP is mediated in part through peripheral 5-HT receptors. Microstructural analysis revealed that 5-HTP and fenfluramine induced a decrease in food intake rate and a reduction in feeding batch size. Xylamidine reversed the effects of 5-HTP on food intake rate and induced a slight increase in feeding batch size itself, thus, the peripheral effect of 5-HTP appears to be to slow food intake rate. No effect of xylamidine on fenfluramine-induced changes in feeding was observed. The results suggest that the appetite suppressant effects of 5-HTP and fenfluramine are differentiated based on the peripheral effects of 5-HTP. The peripheral effects of 5-HTP are distinct from the previously reported 5-HT-induced decreases in feeding batch size and duration. Possible mechanisms underlying the differences in peripheral effects of 5-HT and 5-HTP are discussed.

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-169127

Seganserin	5-HT Receptor	Neurological Disease
Seganserin is an orally active *5-HT* receptor antagonist with a plasma half-life of 26.1 ± 12.9 (S.D.) h. Seganserin can be utilized in neurological research .

HY-118557

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

HY-B0031S

Quetiapine-d4 fumarate	5-HT Receptor Dopamine Receptor	Neurological Disease
Quetiapine-d₄ (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .

HY-100648

Keto Ziprasidone	5-HT Receptor Dopamine Receptor	Neurological Disease
Keto Ziprasidone is an impurity of Ziprasidone . Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist .

HY-156807

LY 367265	Serotonin Transporter 5-HT Receptor	Neurological Disease
LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a **5-HT₂A receptor** antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as *5-HT₁B* (Kᵢ = 490 nM) and *5-HT₁D* (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder .

HY-B1213A

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

HY-17390B

Loxapine hydrochloride	Dopamine Receptor 5-HT Receptor	Neurological Disease
Loxapine hydrochloride is an orally active dopamine inhibitor, **5-HT receptor** antagonist and also a dibenzoxazepine anti-psychotic agent .

HY-103089

LY393558	5-HT Receptor	Neurological Disease
LY393558 is a potent and orally active inhibitor of the *5-HT* transporter and an antagonist of *5-HT1B* and *5-HT1D* receptors. LY393558 increase the extracellular levels of *5-HT* in mice model frontal cortex. LY393558 can be used for researching depression .

HY-19417A

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

HY-G0014

Quetiapine sulfoxide Quetiapine S-oxide	Drug Metabolite	Neurological Disease
Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic . Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist .

HY-101344

Cyanopindolol fumarate	5-HT Receptor	Neurological Disease
Cyanopindolol fumarate is a *5-HT* receptor antagonist .

HY-14542C

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

HY-14542B

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

HY-B0031S2

Quetiapine-d8 fumarate	Isotope-Labeled Compounds 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 .

HY-P3839

Nocistatin	Opioid Receptor	Neurological Disease
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a G_i/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .

HY-W982195

Napamezole hydrochloride	Adrenergic Receptor 5-HT Receptor	Neurological Disease
Napamezole hydrochloride is an orally active α-2 adrenergic receptor antagonist and serotonin (5-HT *Receptor) reuptake inhibitor, with K_i* values of 28 nM and 93 nM for rat α-2 and α-1 adrenergic receptors, respectively. Napamezole hydrochloride can be used for the research of depression .

HY-106605

Flumezapine LY 120363	Dopamine Receptor 5-HT Receptor	Neurological Disease
Flumezapine (LY 120363) is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT *receptor). Flumezapine does not alter the increase in serum cortisol caused by κ-opioid receptor* agonists. Flumezapine inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine can be used in antipsychotic research .

HY-153091

BMY 14802	Adrenergic Receptor 5-HT Receptor Sigma Receptor	Neurological Disease
BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at *serotonin (5-HT) 1A* and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .

Cat. No.	Product Name	Type

HY-Y1191

EEDQ EEDQ	Biochemical Assay Reagents
EEDQ is a carboxylate activator and irreversible antagonist of *5HT2c* receptors. EEDQ reduces [ ³H]β-CIT binding to the dopamine transporter (DAT) in rat caudate-putamen (CPu) homogenates (IC₅₀ = 78.3 μM). EEDQ inhibits contralateral rotation behavior .

HY-75813

2-Aminonicotinaldehyde	Biochemical Assay Reagents
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) .

Cat. No.	Product Name	Target	Research Area

HY-P3839

Nocistatin	Opioid Receptor	Neurological Disease
Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a G_i/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0145

Puerarin Maximum Cited Publications 29 Publications Verification	Structural Classification Flavonoids Pueraria edulis Pampan. Classification of Application Fields Leguminosae Phenols Polyphenols Plants Disease Research Fields Isoflavones Source Classification Cancer	5-HT Receptor
Puerarin is an isoflavone extracted from Pueraria root and is a 5-HT2C receptor antagonist. Puerarin inhibits the dorsal motor nucleus of the vagus (DMV)-vagus nerve pathway, which in turn leads to decreased fat absorption .

HY-N6771

Cyclopiazonic acid 5+ Cited Publications	Alkaloids Structural Classification Microorganisms Pyrrole Alkaloids Classification of Application Fields Other Diseases Disease Research Fields Indole Alkaloids Source Classification	Calcium Channel 5-HT Receptor MDM-2/p53 Apoptosis RSV
Cyclopiazonic acid is an endoplasmic reticulum calcium ATPase (ECAs) inhibitor and human respiratory syncytial virus (RSV) inhibitor (EC₅₀ value of 4.13 μ M), which can reduce the antagonistic effect of 5-HT receptors in rat thoracic aorta, induce p53 dependent cell apoptosis and reproductive toxicity in mouse testes, and inhibit the biological activation of aflatoxin B ^[1][4][5].

HY-N1957

Gamma-Mangostin 2 Publications Verification γ-Mangostin	Xanthones Classification of Application Fields Guttiferae Phenols Polyphenols Garcinia mangostana Linn. Metabolic Disease Plants Disease Research Fields	5-HT Receptor COX Transthyretin (TTR)
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-W010892

Scopolamine hydrobromide trihydrate 20+ Cited Publications Hyoscine hydrobromide trihydrate	Alkaloids Other Alkaloids Datura metel L. Solanaceae Plants Source Classification	mAChR 5-HT Receptor
Scopolamine (Hyoscine) hydrobromide trihydrate is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide trihydrate competitively antagonizes *5-HT₃* receptors with an IC₅₀ of 2.09 μM. Scopolamine hydrobromide trihydrate can induce cognitive and memory deficits in animals. Scopolamine hydrobromide trihydrate can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .

HY-A0019

Paliperidone 3 Publications Verification 9-Hydroxyrisperidone	Natural Products Endogenous metabolite Source Classification	Drug Metabolite Dopamine Receptor 5-HT Receptor Adrenergic Receptor
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-17038

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

HY-N0049

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

HY-N0096

Rotundine (-)-Tetrahydropalmatine; L-Tetrahydropalmatine	Alkaloids Corydalis yanhusuo W. T. Wang Plants Isoquinoline Alkaloids Papaveraceae Source Classification	5-HT Receptor Dopamine Receptor
Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC₅₀s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of *5-HT_1A* with an IC₅₀ of 370 nM.

HY-B2065

Scopolamine hydrochloride 20+ Cited Publications (-)-Scopolamine hydrochloride; Hyoscine hydrochloride	Alkaloids Other Alkaloids Atropa belladonna Linn. Solanaceae Plants Source Classification	mAChR 5-HT Receptor
Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes *5-HT₃* receptors with an IC₅₀ of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .

HY-N0145R

Puerarin (Standard)	Structural Classification Flavonoids Pueraria edulis Pampan. Leguminosae Phenols Polyphenols Plants Isoflavones Source Classification	Reference Standards 5-HT Receptor
Puerarin (Standard) is the analytical standard of Puerarin. This product is intended for research and analytical applications. Puerarin, an isoflavone extracted from Radix puerariae, is a 5-HT2C receptor antagonist.

HY-100971

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

HY-17038A

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

HY-17038B

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

HY-17038R

Agomelatine (Standard) S-20098 (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Reference Standards Melatonin Receptor 5-HT Receptor Endogenous Metabolite
Agomelatine (Standard) is the analytical standard of Agomelatine. This product is intended for research and analytical applications. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with K_is of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively . Agomelatine is a selective **5-HT2C receptor** antagonist with pK_is of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively .

HY-N1957R

Gamma-Mangostin (Standard) γ-Mangostin (Standard)	Structural Classification Xanthones Guttiferae Phenols Polyphenols Garcinia mangostana Linn. Plants	Reference Standards 5-HT Receptor COX Transthyretin (TTR)
Gamma-Mangostin (Standard) is the analytical standard of Gamma-Mangostin. This product is intended for research and analytical applications. 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 [3H] 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-W010892R

Scopolamine hydrobromide trihydrate (Standard) Hyoscine hydrobromide trihydrate (Standard)	Alkaloids Structural Classification Other Alkaloids Datura metel L. Solanaceae Plants Source Classification	mAChR Reference Standards 5-HT Receptor
Scopolamine hydrobromide trihydrate (Standard) is the analytical standard of Scopolamine hydrobromide trihydrate (HY-W010892). This product is intended for research and analytical applications. Scopolamine (Hyoscine) hydrobromide is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrobromide competitively antagonizes *5-HT₃* receptors with an IC₅₀ of 2.09 μM. Scopolamine hydrobromide can induce cognitive and memory deficits in animals. Scopolamine hydrobromide can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .

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 .

HY-A0019R

Paliperidone (Standard) 9-Hydroxyrisperidone (Standard)	Structural Classification Natural Products Endogenous metabolite Source Classification	Drug Metabolite Reference Standards Dopamine Receptor 5-HT Receptor Adrenergic Receptor
Paliperidone (Standard) is the analytical standard of Paliperidone. This product is intended for research and analytical applications. 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-N0049R

Nuciferine (Standard)	Alkaloids other families Plants Source Classification	Reference Standards 5-HT Receptor Dopamine Receptor
Nuciferine (Standard) is the analytical standard of Nuciferine. This product is intended for research and analytical applications. Nuciferine is an antagonist at *5-HT_2A* (IC₅₀=478 nM), *5-HT_2C* (IC₅₀=131 nM), and *5-HT_2B* (IC₅₀=1 μM), an inverse agonist at *5-HT₇* (IC₅₀=150 nM), a partial agonist at D₂ (EC₅₀=64 nM), D₅ (EC₅₀=2.6 μM) and *5-HT₆* (EC₅₀=700 nM), an agonist at *5-HT_1A* (EC₅₀=3.2 μM) and D₄ (EC₅₀=2 μM) receptor.

HY-17038AR

Agomelatine hydrochloride (Standard) S-20098 hydrochloride (Standard)	Structural Classification Alkaloids Other Alkaloids Endogenous metabolite Source Classification	Melatonin Receptor 5-HT Receptor Endogenous Metabolite Reference Standards
Agomelatine (hydrochloride) (Standard) is the analytical standard of Agomelatine (hydrochloride). This product is intended for research and analytical applications. 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-N7541R

Antrodin A (Standard)	Microorganisms Ketones, Aldehydes, Acids Source Classification	HCV Protease Reference Standards
Metoclopramide (Standard) is the analytical standard of Metoclopramide. This product is intended for research and analytical applications. Metoclopramide is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis .

Cat. No.	Product Name	Chemical Structure

HY-15780S1

Brexpiprazole-d8-1

Brexpiprazole-d₈-1 (OPC-34712-d₈-1) is the deuterium labeled Brexpiprazole (HY-15780) . Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (K_i=0.17 nM) and α2C receptors (K_i=0.59 nM) .

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-14940S

Volinanserin-d4 hydrochloride
Volinanserin-d₄ (hydrochloride) is the deuterium labeled Volinanserin hydrochlorid. Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a K_i 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-133111S

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

HY-B0031S1

Quetiapine-d4 hemifumarate
Quetiapine-d₄ (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .

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-B0781S

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

HY-15780S

Brexpiprazole-d8

Brexpiprazole-d₈ (OPC-34712-d₈) is the deuterium labeled Brexpiprazole (HY-15780). Brexpiprazole (OPC-34712), an atypical orally active antipsychotic agent, is a partial agonist of human 5-HT1A and dopamine D_2L receptor with K_is of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a K_i of 0.47 nM. Brexpiprazole also shows potent antagonist activity at human noradrenergic α1B (K_i=0.17 nM) and α2C receptors (K_i=0.59 nM) ^.

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-14541S

Olanzapine-d3
Olanzapine-d₃ (LY170053-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 .

HY-B0031S

Quetiapine-d4 fumarate
Quetiapine-d₄ (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects .

HY-B0716S2

Urapidil-d4
Urapidil-d₄ is the deuterium labeled Urapidil . Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist .

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-A0019S

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

HY-17038S2

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

HY-133152S

Brexpiprazole S-oxide-d8

Brexpiprazole S-oxide-d₈ (DM-3411 D₈) is a deuterium labeled Brexpiprazole S-oxide (HY-133152). 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 K_is 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-17410S

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

HY-13575S1

Blonanserin-d5
Blonanserin-d₅ (AD-5423-d₅) is a deuterium labeled Blonanserin (HY-13575). Blonanserin is a dopamine D2/5-HT2 receptor antagonist and an atypical antipsychotic .

HY-B0031S2

Quetiapine-d8 fumarate

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

HY-70050AS

Alosetron-d3
Alosetron-d₃ is a deuterium labeled Alosetron. Alosetron is a serotonin 5HT3-receptor antagonist .

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-B0032AS

Lurasidone-d8
Lurasidone-d₈ is deuterium labeled Lurasidone. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.

HY-17637S2

Lumateperone-d4

Lumateperone-d₄ (ITI-007-d₄) is deuterium labeled Lumateperone. Lumateperone (ITI-007) is an orally active 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 for the study of schizophrenia and bipolar depression .

HY-B0002S1

Ondansetron-d6 hydrochloride
Ondansetron-d₆ (hydrochloride) is the deuterium labeled Ondansetron hydrochloride . Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy .

HY-17038S1

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

HY-B2169S2

Melperone-d4 hydrochloride

Melperone-d₄ hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with K_ds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with K_d values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .

HY-B0352S3

Mirtazapine-d4 hydrochloride
Mirtazapine-d₄ hydrochloride is deuterated labeled Mirtazapine (HY-B0352). Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a *5-HT₂, 5-HT₃, histamine H1 receptor* and α2-adrenoceptor antagonist with pK_i values of 8.05, 8.1, 9.3 and 6.95, respectively .

HY-A0019AS

Paliperidone palmitate-d4

Paliperidone palmitate-d₄ (9-Hydroxyrisperidone palmitate-d₄) is the deuterium labeled Paliperidone palmitate (HY-A0019A). Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia .

HY-15394S

(Rac)-Rotigotine-d7 hydrochloride

(Rac)-Rotigotine-d₇ (hydrochloride) is deuterium labeled (Rac)-Rotigotine (hydrochloride). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.

HY-A0007S

Rotigotine-d7 hydrochloride

Rotigotine-d₇ (N-0923-d₇) hydrochloride is the deuterium labeled Rotigotine(HY-75502). Rotigotine is a potent dopamine receptor agonist with K_i values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.

HY-W010892S

Scopolamine-d3 hydrobromide

Scopolamine-d₃ hydrobromide is the deuterium labeled Scopolamine hydrobromide (HY-B2065). Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT₃ receptors with an IC₅₀ of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc .

HY-14542S

Ziprasidone-d8
Ziprasidone-d₈8 is deuterium labeled Ziprasidone, which is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.

HY-B1213S

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

HY-B0982S

Pindolol-d7
Pindolol-d₇ (LB-46-d7) is the deuterium labeled Pindolol. Pindolol (LB-46) is the antagonist for 5-HT 1A (K_i=33 nM) and 5-HT 1B. Pindolol is the antagonist for β1/β2-adrenergic receptor. Pindolol exhibits anti-anxiety and antidepressant effects .

HY-16567S

Asenapine-13C,d3 hydrochloride
Asenapine- ¹³C,d₃ (hydrochloride) is the ¹³C- and deuterium labeled Asenapine (hydrochloride). Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.

HY-G0014S

Quetiapine Sulfoxide-d8
Quetiapine Sulfoxide-d₈ is the deuterium labeled Quetiapine sulfoxide. Quetiapine sulfoxide (Quetiapine S-oxide) is a main metabolite of Quetiapinem. Quetiapine is a second-generation antipsychotic . Quetiapine is a 5-HT receptors agonist and a dopamine receptor antagonist .

HY-B0031S3

Quetiapine-d8 hemifumarate

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

HY-B0031S4

Quetiapine hemifumarate-d8

Quetiapine (hemifumarate)-d₈ 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 .

HY-B0031S5

Quetiapine-d4-1 fumarate

Quetiapine-d₄-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

HY-14544AS

Quetiapine-d4 hydrochloride

Quetiapine-d₄ (hydrochloride) (ICI204636-d₄ (hydrochloride)) is deuterium labeled Quetiapine. Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC₅₀ of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC₅₀ of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pK_is of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects .

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-106605S

Flumezapine-d8 hydrochloride

Flumezapine-d₈ (LY 120363-d₈) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.

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-70050CS

Alosetron-d3 hydrochloride
Alosetron-d₃ (hydrochloride) is deuterium labeled Alosetron, which is a serotonin 5HT3-receptor antagonist.

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-B0781S1

Promethazine-d3 hydrochloride

Promethazine-d₃ (hydrochloride) is deuterium labeled Promethazine (hydrochloride). 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-W742404

Bopindolol-d9

Bopindolol-d₉ ((±)-Bopindolol-d₉) is the deuterium labeled Bopindolol (HY-B1562). Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.

HY-B0115S

Pizotyline-d3
Pizotyline-d₃ is deuterated labeled Pizotifen (HY-B0115). Pizotifen (Pizotyline) is a potent *5-HT₂* receptor antagonist, with a high affinity for *5-HT_1C* binding site.

HY-14153AS

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

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