5-HT Receptor
Serotonin Receptor; 5-hydroxytryptamine Receptor
5-HT receptors (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. Type: 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, as well as many hormones. The serotonin 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.
5-HT Receptor Isoform Specific Products
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5-HT Receptor
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5-HT1 Receptor
(456)
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5-HT2 Receptor
(491)
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5-HT3 Receptor
(35)
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5-HT4 Receptor
(19)
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5-HT5 Receptor
(14)
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5-HT6 Receptor
(86)
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5-HT7 Receptor
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All Product Categories
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5-HT Receptor Inhibitors
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5-HT Receptor Agonists
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5-HT Receptor Antagonists
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5-HT Receptor Activators
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5-HT Receptor Modulators
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5-HT Receptor Inducers
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5-HT Receptor Controls
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5-HT Receptor Ligands
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5-HT Receptor Related Products (1775)
Related Products (1775)
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Antibodies (1)
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Related Compound Screening Libraries (1)
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5-HT Receptor Isoform Comparison
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Paliperidone-d4
0 ImagesCat. No.: HY-A0019SCAS No.: 1020719-55-4Paliperidone-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.
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Agomelatine-d4
0 ImagesCat. No.: HY-17038S1CAS No.: 1079389-44-8Synonyms: S-20098-d4Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. 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.
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Iloperidone-d3
0 ImagesCat. No.: HY-17410SCAS No.: 1071167-49-1Iloperidone-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.
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Cyclobenzaprine-d3 hydrochloride
0 ImagesCat. No.: HY-B0740SCAS No.: 1184983-42-3Synonyms: MK130-d3 hydrochlorideCyclobenzaprine-d3 (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
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Cyamemazine-d6
0 ImagesCat. No.: HY-14264SCAS No.: 1216608-24-0Cyamemazine-d6 is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.
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Dolasetron Mesylate hydrate (Standard)
0 ImagesCat. No.: HY-B0750BRCAS No.: 878143-33-0Synonyms: MDL-73147EF hydrate (Standard)Dolasetron Mesylate hydrate (MDL-73147EF hydrate) (Standard) is the analytical standard of Dolasetron Mesylate hydrate (HY-B0750B). This product is intended for research and analytical applications. Dolasetron Mesylate hydrate is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
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MS 245 oxalate
0 ImagesCat. No.: HY-103113CAS No.: 275363-58-1MS 245 oxalate is a potent antagonist of 5-HT6 receptor with a Ki of 2 nM.
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DV-7028 hydrochloride
0 ImagesCat. No.: HY-103116CAS No.: 133364-62-2DV-7028 is a selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist.
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LY 367265
0 ImagesCat. No.: HY-156807CAS No.: 210751-39-6LY 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.
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RS-102221
0 ImagesRS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats.
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Tropisetron Hydrochloride (Standard)
0 ImagesSynonyms: SDZ-ICS-930 (Standard)Tropisetron (Hydrochloride) (Standard) is the analytical standard of Tropisetron (Hydrochloride). Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation.
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SB-656104
0 ImagesCat. No.: HY-124135CAS No.: 446020-51-5SB-656104 is a potent antagonist of 5-HT7 receptor, with the pKi of 8.70, blocking 5-carboxamidotryptamine (5-CT) stimulated adenylyl cyclase activity.
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Etoperidone hydrochloride
0 ImagesCat. No.: HY-106617ACAS No.: 57775-22-1Etoperidone hydrochloride, an antidepressant agent, is an orally active serotonin and nor-adrenaline re-uptake antagonist. Etoperidone hydrochloride shows Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively.
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Isamoltan hydrochloride
0 ImagesCat. No.: HY-19578ACAS No.: 99740-06-4Synonyms: (±)-Isamoltane hydrochlorideIsamoltan ((±)-Isamoltane) hydrochloride is a selective antagonist of 5-HT1B receptor, with an IC50 of 39 nM for inhibits the binding of [125I]ICYP to 5-HT1B recognition sites in rat brain membranes. Isamoltan hydrochloride is also a β-adrenoceptor ligand, with an IC50 of 8.4 nM. Isamoltan hydrochloride shows anxiolytic activity.
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AVN-211
0 ImagesCat. No.: HY-105998CAS No.: 1173103-84-8AVN-211 (CD-008-0173) is a selective and orally active 5HT6R antagonist with an IC50 of 2.34 nM and a Ki of 1.09 nM. AVN-211 exhibits 5K-fold higher 5HT6R selectivity over other 65 receptors, enzymes, and ion channels. AVN-211 significantly improves cognitive and anxiety behaviors in various AD animal models, and has good safety profiles. AVN-211 can be used for the study of Alzheimer's dementia.
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Ro4368554
0 ImagesCat. No.: HY-135456CAS No.: 478082-99-4Ro4368554 is a brain-penetrant and selective 5-HT6 antagonist that reverses memory deficits induced by scopolamine and tryptophan depletion. Ro4368554 can be utilized in research related to memory deficits.
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S18327
0 ImagesCat. No.: HY-165527CAS No.: 200398-40-9S18327 is a multi-target antipsychotic agent. S18327 exerts its efficacy by acting on multiple neurotransmitter systems in the brain, and it has antagonistic effects on dopamine receptors (particularly the D2 receptor) and 5-hydroxytryptamine 2A receptors (5-HT2A receptor). S18327 can counteract excessive dopamine activity and hypo-function of glutamate. S18327 exhibits a multi-parameter pharmacological profile that is highly similar to that of Clozapine (HY-14539). S18327 can produce the same discriminative stimulus as Clozapine, improve cognitive filtering deficits associated with schizophrenia, and display anxiolytic properties. S18327 has relatively weak affinity for histaminergic receptors and muscarinic receptors, which avoids the side effects of Clozapine.
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Dimethothiazine mesylate
0 ImagesCat. No.: HY-A0157ACAS No.: 13115-40-7Synonyms: Dimetotiazine mesylate; Fonazine mesylateDimethothiazine mesylate is an orally active tricyclic anti-histamine, anti-5-HT agent with a high activity against decerebrate rigidity, a little sedative activity and little soporific action. Dimethothiazine mesylate can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine mesylate can be used to research hemicrania and spasticity.
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Trimipramine (Standard)
0 ImagesCat. No.: HY-B1213ARCAS No.: 739-71-9Trimipramine (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.
