1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-14546R
    Aripiprazole (Standard)
    Agonist
    Aripiprazole (Standard) is the analytical standard of Aripiprazole. This product is intended for research and analytical applications. Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.
    Aripiprazole (Standard)
  • HY-103104
    Fananserin
    Antagonist 99.97%
    Fananserin (RP 62203) is an orally bioavailable, potent and selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist, with a Ki of 0.37 nM for the rat 5-HT2A receptor. Fananserin also is a selective dopamine D4 receptor antagonist, with a Ki of 2.93 nM for the human dopamine D4 receptor.
    Fananserin
  • HY-U00286
    5-HT2A antagonist 1
    Antagonist
    5-HT2A antagonist 1 is a 5-HT2A antagonist extracted from patent US5728835A and JP 1007727. 5-HT2A antagonist 1 may be useful in treatment of gastrointestinal disorders circulatory disorders.
    5-HT2A antagonist 1
  • HY-103108
    CJ033466
    Agonist 98.29%
    CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect.
    CJ033466
  • HY-116795
    5-Methoxy-α-ethyltryptamine
    98.91%
    5-Methoxy-α-ethyltryptamine is a tryptamine psychoactive substance, which has nerve stimulated effect.
    5-Methoxy-α-ethyltryptamine
  • HY-14149A
    Cisapride monohydrate
    Agonist 99.87%
    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.
    Cisapride monohydrate
  • HY-119061
    SB357134
    Antagonist
    SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats.
    SB357134
  • HY-W982195
    Napamezole hydrochloride
    Inhibitor 98.97%
    Napamezole hydrochloride is an orally active α-2 adrenergic receptor antagonist and serotonin (5-HT Receptor) reuptake inhibitor, with Ki 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.
    Napamezole hydrochloride
  • HY-W342283
    Diminazene
    Activator
    Diminazene is an antiparasitic agent widely used to treat parasitic diseases caused by hemoparasites (such as trypanosomes and babesia). Diminazene acts as an ACE2 activator and exerts cardiovascular protective effects by activating the ACE2/Ang-(1-7)/Mas receptor axis. By regulating gut microbiota-tryptophan metabolism, Diminazene inhibits the activation of core inflammatory signaling pathways including MAPK, STAT and NF-κB, increases central 5-HT levels, and suppresses splenic TNF-α production, thereby alleviating systemic inflammation.
    Diminazene
  • HY-101377A
    R(+)-8-OH-DPAT hydrobromide
    Agonist 99.30%
    R(+)-8-OH-DPAT ((R)-8-Hydroxy-2-dipropylaminotetralin) hydrobromide is a potent 5-HT1A agonist. R(+)-8-OH-DPAT potentiates SUL (HY-B1059)-induced dopamine (DA) release in the medial prefrontal cortex (mPFC).
    R(+)-8-OH-DPAT hydrobromide
  • HY-179579
    TMU4142
    Agonist 98.93%
    TMU4142 is a selective 5-HT1a agonist with high GoA activity. TMU4142 has weak Gi3 activity, can elicit rapid antidepressant like effects without triggering significant activation of dorsal raphe nucleus (DRN) 5-HT1a R autoreceptors or serotonergic neuron firing. TMU4142 demonstrates fast-acting efficacy in mouse models of depression. TMU4142 can be used for antidepressants research.
    TMU4142
  • HY-A0021C
    (R,R)-Palonosetron Hydrochloride
    99.61%
    (R,R)-Palonosetron Hydrochloride is the active enantiomer of Palonosetron.
    (R,R)-Palonosetron Hydrochloride
  • HY-100166
    AP521
    Agonist 98.96%
    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
    AP521
  • HY-U00373
    Revexepride
    Agonist 99.84%
    Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.
    Revexepride
  • HY-103140
    Ro60-0175 fumarate
    Agonist 99.47%
    Ro60-0175 fumarate is a potent and selective agonist of 5-HT2C receptor.
    Ro60-0175 fumarate
  • HY-10861
    D3/5-HT receptor modulator-1
    Modulator 99.75%
    D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile.
    D3/5-HT receptor modulator-1
  • HY-103154
    SB228357
    Antagonist 99.43%
    SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects.
    SB228357
  • HY-N2125R
    Parishin C (Standard)
    Agonist
    Parishin C (Standard) is the analytical standard of Parishin C (HY-N2125). This product is intended for research and analytical applications. Parishin C is a brain-penetrant major bioactive component found in Gastrodia elata Blume. Parishin C is a 5-HT1A receptor agonist with an EC50 of 34 nM. Parishin C has antipsychotic and neuroprotective effects. Parishin C protects against Aβ-induced long-term potentiation damage and NMDA receptor current impairment. Parishin C reduces oxidative stress, pro-inflammatory cytokine levels, caspase activity, brain water content, and cerebral infarct volume; increases antioxidant enzyme activity and BDNF levels; improves nerve function and histopathological brain damage. Parishin C attenuates phencyclidine-induced immobility time increases, sociability deficits, and visual recognition memory impairment. Parishin C can be used for the research of ischemic stroke, Alzheimer's disease, and schizophrenia-like psychosis.
    Parishin C (Standard)
  • HY-14261S
    Vilazodone-d8
    Inhibitor 99.0%
    Vilazodone-d8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
    Vilazodone-d<sub>8</sub>
  • HY-B0197
    Naratriptan
    Agonist 98.05%
    Naratriptan is an orally active and selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.
    Naratriptan
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