2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

Related Products

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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:

5-HT Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-18137
    PF-04995274
    		Agonist 99.75%
    PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
    PF-04995274
  • HY-145393
    5-HT2A receptor agonist-1
    		Agonist 99.94%
    5-HT2A receptor agonist-1 (Compound 3) is a selective 5-HT2A receptor agonist with the EC50 of 5.54 nM. 5-HT2A receptor agonist-1 can be used for the research of mood disorders.
    5-HT2A receptor agonist-1
  • HY-14690
    Ecopipam
    		Antagonist 99.77%
    Ecopipam (SCH 39166) is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam can be used for the research of schizophrenia and obesity.
    Ecopipam
  • HY-100769
    Hypidone hydrochloride
    		Agonist 99.73%
    Hypidone hydrochloride (YL0919) is an orally active antidepressant agent with dual activity as a highly seletive 5-HT uptake blocker and an effective 5-HT1A receptor agonist (Ki=0.19 nM). Hypidone hydrochloride inhibits the uptake of [3H]-5-HT into rat cerebral cortical synaptosomes and HEK293 cells with IC50s of 1.78 nM and 1.93 nM, respectively. Hypidone hydrochloride shows remarkable antidepressant effects in animal models and has the poential for the investigation of depressive disorder.
    Hypidone hydrochloride
  • HY-100656
    Desmethyl cariprazine
    		Antagonist 98.08%
    Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
    Desmethyl cariprazine
  • HY-103099
    SB-399885 hydrochloride
    		Antagonist 98.33%
    SB-399885 hydrochloride is a 5-HT6 receptor antagonist.
    SB-399885 hydrochloride
  • HY-108256
    Melitracen hydrochloride
    		Inhibitor 99.80%
    Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.
    Melitracen hydrochloride
  • HY-75813
    2-Aminonicotinaldehyde
    		99.98%
    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).
    2-Aminonicotinaldehyde
  • HY-109157
    Ralmitaront
    		Agonist 99.92%
    Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.
    Ralmitaront
  • HY-15543A
    CP-809101 hydrochloride
    		Agonist 98.61%
    CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.
    CP-809101 hydrochloride
  • HY-B0527AR
    Amitriptyline hydrochloride (Standard)
    		Inhibitor
    Amitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
    Amitriptyline hydrochloride (Standard)
  • HY-153912
    5-HT2A receptor agonist-3
    		Agonist 98.53%
    5-HT2A receptor agonist-3 ((S,S)-9b) is a 5-HT2A receptor agonist with a Ki of 2.5 nM for human 5-HT2A receptor. 5-HT2A receptor agonist-3 shows 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor.
    5-HT2A receptor agonist-3
  • HY-B0115
    Pizotifen
    		Antagonist 99.63%
    Pizotifen (Pizotyline) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen
  • HY-121301
    Amperozide
    		Antagonist 98.81%
    Amperozide is an atypical antipsychotic that acts as an antagonist of the 5-HT2 receptor with a Ki value of 26 nM. Amperozide has a low affinity for D2 receptors.
    Amperozide
  • HY-B1107
    Naftidrofuryl oxalate
    		Antagonist 99.94%
    Naftidrofuryl oxalate (Nafronyl oxalate salt) is an orally active 5-HT2 receptor antagonist. Naftidrofuryl oxalate selectively blocks vascular and platelet 5-HT2 receptors, inhibiting Serotonin (HY-B1473A)-induced vasoconstriction, platelet aggregation, and vascular smooth muscle cell proliferation. Naftidrofuryl oxalate can be used for the research of intermittent claudication, peripheral occlusive arterial disease, and critical limb ischaemia.
    Naftidrofuryl oxalate
  • HY-B0061
    Tandospirone citrate
    		Agonist 99.92%
    Tandospirone (SM-3997) citrate is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone citrate has anxiolytic and antidepressant activities. Tandospirone citrate can be used for the research of the central nervous system disorders and the underlying mechanisms.
    Tandospirone citrate
  • HY-14539S2
    Clozapine-d4
    		Modulator 99.80%
    Clozapine-d4 is the deuterium labeled Clozapine. Clozapine is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors.
    Clozapine-d<sub>4</sub>
  • HY-14339
    Intepirdine
    		Antagonist 99.02%
    Intepirdine (SB742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63; exhibits >100-fold selectivity over other receptors.
    Intepirdine
  • HY-W010869
    GR 55562 hydrochloride
    		Antagonist 98.0%
    GR 55562 hydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 hydrochloride can be used for the research of nerve disease.
    GR 55562 hydrochloride
  • HY-101357A
    CP 93129 dihydrochloride
    		Agonist 98.01%
    CP 93129 dihydrochloride is a potent 5HT1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research.
    CP 93129 dihydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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