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-B0020R
    Tropisetron Hydrochloride (Standard)
    Antagonist
    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.
    Tropisetron Hydrochloride (Standard)
  • HY-186169A
    S-MDDMA
    S-MDDMA is the S-enantiomer of (R,S)-MDDMA (HY-186169B), and mediates serotonin release from cells expressing SERT.
    S-MDDMA
  • HY-124135
    SB-656104
    Antagonist
    SB-656104 is a potent antagonist of 5-HT7 receptor, with the pKi of 8.70, blocking 5-carboxamidotryptamine (5-CT) stimulated adenylyl cyclase activity.
    SB-656104
  • HY-106617A
    Etoperidone hydrochloride
    Antagonist
    Etoperidone 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.
    Etoperidone hydrochloride
  • HY-B0901S1
    Bromperidol-d4-1
    Inhibitor
    Bromperidol-d4-1 is deuterium labeled Bromperidol.
    Bromperidol-d<sub>4</sub>-1
  • HY-117119
    VER-3323
    Agonist
    VER-3323 is an oral active 5-HT2C agonist and belongs to the class of indoline analogs. VER-3323 reduces food intake in rats by inducing swallowing dysfunction, with no significant impact on energy expenditure generated through thermogenesis or exercise. VER-3323 can be utilized in obesity research.
    VER-3323
  • HY-19578A
    Isamoltan hydrochloride
    Antagonist
    Isamoltan ((±)-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.
    Isamoltan hydrochloride
  • HY-B1562C
    Bopindolol fumarate
    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.
    Bopindolol fumarate
  • HY-167675
    R-137696
    Agonist
    R-137696 is an orally active serotonin-1A (5-HT1A) receptor agonist which relaxes the proximal stomach. R-137696 can be utilized in research related to functional dyspepsia.
    R-137696
  • HY-182472
    AL-38022A
    Agonist
    AL-38022A is a potent and selective 5-HT2 receptor agonist (Ki ≤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 [Ca2+]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.
    AL-38022A
  • HY-W011040
    LY320135
    Modulator
    LY320135 is a potent and selective antagonist of CB1 receptor, with a Ki of 141 nM. LY320135 also binds to 5-HT2 and muscarinic receptors with Kis of 6.4 μM and 2.1 μM, respectively. LY320135 exhibits neuroprotective effect.
    LY320135
  • HY-105998
    AVN-211
    Antagonist
    AVN-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.
    AVN-211
  • HY-B1473S2
    Serotonin-13C,D4
    Serotonin-13C,D4 (5-Hydroxytryptamine-13C,D4) is a 13C- and deuterated labeled Serotonin (HY-B1473A). Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
    Serotonin-<sup>13</sup>C,D<sub>4</sub>
  • HY-19029
    SDZ 208-912
    Agonist
    SDZ 208-912 is a dual-action 5-HT1A/2 receptor agonist and dopamine D1 receptor antagonist. SDZ 208-912 exhibits partial dopamine agonism and atypical neurosedative effects in rodent models. SDZ 208-912 can be used in research on neurological disorders such as schizophrenia.
    SDZ 208-912
  • HY-B1115S
    Buspirone-d8 hydrochloride
    Agonist
    Buspirone-d8 (hydrochloride) is the deuterium labeled Buspirone hydrochloride. Buspirone hydrochloride is an anxiolytic psychotropic agent, is used to treat generalized anxiety disorder (GAD).
    Buspirone-d<sub>8</sub> hydrochloride
  • HY-122537
    Arotinolol hydrochloride
    Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol hydrochloride also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol hydrochloride is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
    Arotinolol hydrochloride
  • HY-100426
    Osemozotan
    Agonist
    Osemozotan (MKC242 free base) acts as an agonist for the 5-HT(1A) receptor.
    Osemozotan
  • HY-135456
    Ro4368554
    Antagonist
    Ro4368554 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.
    Ro4368554
  • HY-155206
    (+)-OSU6162
    Agonist 98.27%
    (+)-OSU6162 is an stabilizer on dopaminergic and serotonergic brain signaling. (+)-OSU6162 is a partial agonist of 5-HT2A receptor. (+)-OSU6162 can be used for neurological research.
    (+)-OSU6162
  • HY-165527
    S18327
    Antagonist
    S18327 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.
    S18327
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