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5-HT receptor subtypes

" in MedChemExpress (MCE) Product Catalog:

By Targets:	5-HT Receptor (26) Adrenergic Receptor (8) Akt (2) Dopamine Receptor (2) Drug Metabolite (2) Epigenetic Reader Domain (1) FOXO (1) GABA Receptor (1) Isotope-Labeled Compounds (2) Liposome (1) mAChR (2) Phosphatase (1) Reference Standards (5) Renin (3) Ribosomal S6 Kinase (RSK) (1) Serotonin Transporter (2)
By Research Areas:	Cancer (2) Cardiovascular Disease (4) Inflammation/Immunology (3) Metabolic Disease (1) Neurological Disease (26)

Inhibitors & Agonists

Screening Libraries

Isotope-Labeled Compounds

Targets Recommended: 5-HT Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-103100

SB-699551 1 Publications Verification	5-HT Receptor Epigenetic Reader Domain Akt Ribosomal S6 Kinase (RSK) FOXO	Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
SB-699551 is a selective and brain penetrant **5-HT5A receptor antagonist with a pK_i** of 8.2 nM. SB-699551 shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 can be used for the research of anxiety, breast cancer, and Alzheimer's disease .

HY-101630

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

HY-B1562B

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

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-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-W014208

NGX-267 AF-267B	mAChR	Others
NGX-267 is a selective agonist of the actin M1 receptor, which has high selectivity among the five actin receptor subtypes, especially for the M1 receptor rather than the M3 receptor. NGX-267 also has significant differences in affinity for dopamine D2 and 5-HT2B receptors .

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-124296

2C-TFM hydrochloride	5-HT Receptor	Neurological Disease
2C-TFM hydrochloride is a ,5-dimethoxyphenethylamines compound with a para-trifluoromethyl substitution. 2C-TFM hydrochloride is a potent agonist of the **5-HT receptor** subtypes 5-HT2A and 5-HT2C .

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-175532

M4 mAChR Modulator-2	mAChR	Neurological Disease
M4 mAChR Modulator-2 is an orally active, selective, brain-penetrant positive allosteric modulator (PAM) of the M4 muscarinic acetylcholine receptor (M4 mAChR) (EC₅₀ = 513 nM). M4 mAChR Modulator-2 exhibits high target selectivity, showing negligible affinity and low inhibition rates for non-target receptors (D1R/D2R/D3R, 5-HT subtypes, κ/δ/μ opioid receptors, H1, M1/M2) while specifically binding to M4 mAChR with a K_i of 377 nM and an inhibition rate of 62.8%. M4 mAChR Modulator-2 reverses Dizocilpine (MK-801) (HY-15084B)-induced hyperlocomotion in mice. M4 mAChR Modulator-2 can be used for the study of schizophrenia

HY-133790

Palonosetron N-oxide	5-HT Receptor	Neurological Disease
Palonosetron N-oxide is a metabolite of the serotonin (5-HT) receptor subtype 5-HT3 antagonist Palonosetron (HY-A0018).

HY-117792

LY314228	5-HT Receptor	Inflammation/Immunology
LY314228 is an aminoguanidine *5-HT2* antagonist with relative selectivity for *5-HT2A receptors* (IC50: 147.9 nM). The Ki values of LY314228 targeting different 5-HT subtypes are 65 nM (5-HT 2A), 1214 nM (5-HT 2B), and 168 nM (5-HT 2C), respectively. LY314228 is an effective inhibitor of 5-HT-induced paw edema in rats with an ED50 of 6.4 mg/kg in ovariectomized female rats. .

HY-W700240

Triazolomethylindole-3-acetic acid	5-HT Receptor	Neurological Disease
Triazolomethylindole-3-acetic acid is a metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist Rizatriptan HY-B0206).

HY-W740014

N-Desmethyl Zolmitriptan 183C91; DZT	5-HT Receptor	Neurological Disease
N-Desmethyl Zolmitriptan (183C91; DZT) is the active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist Zolmitriptan (HY-B0229). N-Desmethyl Zolmitriptan (183C91; DZT) is an agonist of 5-HT1B receptors and induces constriction in isolated human cerebral arteries (EC50=100 nM).

HY-135774R

6-Hydroxybenzbromarone (Standard)	Reference Standards Drug Metabolite Phosphatase	Cardiovascular Disease
1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard) is the analytical standard of 1-(Carboxymethyl)cyclohexanecarboxylic acid. This product is intended for research and analytical applications. 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-W016194R

1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard) 1-Carboxycyclohexaneacetic acid (Standard); Gabapentin Impurity E (Standard); Gabapentin Related Compound E (Standard)	5-HT Receptor Reference Standards	Neurological Disease
1-(Carboxymethyl)cyclohexanecarboxylic acid (Standard) is the analytical standard of 1-(Carboxymethyl)cyclohexanecarboxylic acid. This product is intended for research and analytical applications. 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-100057

BMY 28674 6-Hydroxybuspirone; 6'-Hydroxybuspirone; BMS 528215	5-HT Receptor Drug Metabolite Dopamine Receptor	Neurological Disease
BMY 28674 (6-Hydroxybuspirone) is the active metabolite of the anxiolytic buspirone (HY-B1115A) and is metabolized by CYP3A4.4. BMY 28674 binds to the serotonin (5-HT) receptor subtype *5-HT1A* in the rat hippocampus and dorsal raphe (EC₅₀s are 4 and 1 μM, respectively) and is an antagonist of dopamine D2, D3, and D4 receptors (IC₅₀s are 3.1, 4.9, and 0.85 μM, respectively). BMY 28674 also inhibits organic cation transporter 1 (OCT1), OCT2, and OCT3 expressing human transporters in S2 proximal tubule cells in a concentration-dependent manner.

HY-B1562C

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

HY-B1562

Bopindolol (±)-Bopindolol	Adrenergic Receptor Renin 5-HT Receptor	Cardiovascular Disease Neurological Disease
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-101630R

Deramciclane (Standard) EGIS-3886 (Standard)	Reference Standards 5-HT Receptor	Neurological Disease
Deramciclane (Standard) is the analytical standard of Deramciclane. This product is intended for research and analytical applications. Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.

HY-W742404

Bopindolol-d9 (±)-Bopindolol-d₉	Isotope-Labeled Compounds Adrenergic Receptor 5-HT Receptor	Neurological Disease
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-18596

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

HY-32329S

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

HY-32329R

Setiptiline (Standard) Org-8282 (Standard)	5-HT Receptor Adrenergic Receptor Reference Standards	Neurological Disease
Setiptiline (Standard) is the analytical standard of Setiptiline. This product is intended for research and analytical applications. 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-32329AR

Setiptiline maleate (Standard) MO-8282 (Standard)	5-HT Receptor Reference Standards	Neurological Disease
Setiptiline (maleate) (Standard) is the analytical standard of Setiptiline (maleate). This product is intended for research and analytical applications. Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .

HY-136700

SB-699551 free base	5-HT Receptor Akt	Neurological Disease Cancer
SB-699551 free base is a selective and brain penetrant **5-HT5A receptor antagonist with a pK_i** of 8.2 nM. SB-699551 free base shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 free base disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 free base can be used for the research of anxiety, breast cancer, and Alzheimer's disease .

HY-W1130456

Lipid TD5	Liposome	Inflammation/Immunology
Lipid TD5 is an ionizable cationic lipid with a pK_a of 7.3. Lipid TD5 can be used to generate lipid nanoparticles (LNPs) to deliver mRNA in vitro and in vivo. Lipid TD5 LNPs can undergo endocytosis in a 5-HT receptor subtype 1A-dependent manner in primary mouse astrocytes .

HY-182472

AL-38022A	5-HT Receptor	Neurological Disease
AL-38022A is a potent and selective **5-HT₂ receptor agonist (K_i ≤2.2 nM), but a significantly lower (>100-fold less) affinity for other 5-HT receptors*. AL-38022A potently stimulates functional responses via 5-HT₂* receptor subtypes including [Ca ²⁺]_i mobilization and tissue contractions with apparently similar potencies and intrinsic activities. AL-38022A fully generalizes to the (±)-1-(2,5-dimethoxy 4-methylphenyl)-2-aminopropane hydrochloride (DOM) stimulus in drug discrimination paradigms. AL-38022A can be used for the glaucoma research .

HY-180372

CSP-2503	5-HT Receptor Adrenergic Receptor GABA Receptor Serotonin Transporter Dopamine Receptor	Neurological Disease
CSP-2503 is a potent and selective 5-HT_1A receptor agonist , with an EC₅₀ of 0.15 μM and a K_i of 4.1 nM. CSP-2503 exhibits excellent selectivity over α1-adrenoceptors (K_i > 1000 nM), 5-HT₄ receptors, and benzodiazepine receptors. CSP-2503 inhibits cAMP increase in vitro and exhibits anxiolytic activity in vivo. CSP-2503 can be used for the research of anxiety-related disorders .

Cat. No.	Product Name

HY-L121

5-HT Receptor Compound Library	405 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 405 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

5-HT Receptor Compound Library

405 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 405 5-HT receptor inhibitors and activators, which can be used for neuropsychiatric disorders drugs discovery.

Cat. No.	Product Name	Chemical Structure

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.

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-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 .

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 .

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