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-110024
    S-14506 hydrochloride
    		Agonist 98.64%
    S-14506 hydrochloride is a potent 5-HT1A agonist, as well as 5-HT2A/2C antagonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent.
    S-14506 hydrochloride
  • HY-101367A
    GR 55562 dihydrochloride
    		Antagonist 99.0%
    GR 55562 dihydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 dihydrochloride can be used for the research of nerve disease.
    GR 55562 dihydrochloride
  • HY-101709
    Ricasetron
    		Antagonist 98.62%
    Ricasetron (BRL-46470) is a selective and orally active 5-HT3 receptor antagonist. Ricasetron displays little or no affinity for a variety of other neurotransmitter receptors. Ricasetron has anxiolytic and antiemetic effects.
    Ricasetron
  • HY-156532C
    (-)-5-HT2C agonist-3
    		Agonist
    (-)-5-HT2C agonist-3 (compound (-)-19) is a 5-HT2C selective agonist with Gq signaling preference, with EC50 values for 5-HT2 receptors of 5-HT2C: 103 nM; 5-HT2B: 570 nM; 5-HT2A: 72 nM. (-)-5-HT2C agonist-3 can be used in antipsychotic research.
    (-)-5-HT2C agonist-3
  • HY-103112
    SB 243213 hydrochloride
    		Antagonist 98.84%
    SB 243213 hydrochloride is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 hydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.
    SB 243213 hydrochloride
  • HY-14940A
    (S)-Volinanserin
    		Antagonist 99.84%
    (S)-Volinanserin is an isform of Volinanserin (HY-14940). Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
    (S)-Volinanserin
  • HY-133024
    Flumexadol
    		Agonist 99.86%
    Flumexadol is a selective and affinity 5-HT2C receptor agonist with a Ki of 25 nM for the (+)-enantiomer of Flumexadol, and is 40-fold selective over the 5-HT2A receptor. Flumexadol is an orally active non-narcotic analgesic.
    Flumexadol
  • HY-103147
    Mesulergine hydrochloride
    		Antagonist
    Mesulergine (CU32-085) hydrochloride is a potent 5-HT2C antagonist and dopamine (DA) agonist. Mesulergine hydrochloride presentes hyperphagia. Mesulergine hydrochloride has the potential for the research of cognitive processes.
    Mesulergine hydrochloride
  • HY-103130
    EMD386088
    		Agonist 99.06%
    EMD386088 is a potent and selective 5-HT6 receptor (5-HT6R) agonist with an EC50 of 1.0 nM. EMD-386088 is inactive against other HT receptors except 5-HT3R (IC50 of 34 nM). EMD386088 regulates the activity of ERK1/2. EMD386088 has the potential for the research of alzheimer's disease (AD) and schizophrenia.
    EMD386088
  • HY-A0077S1
    Perphenazine-d4
    		98.83%
    Perphenazine-d4 is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
    Perphenazine-d<sub>4</sub>
  • HY-116790
    (-)-Penbutolol
    		Antagonist 99.74%
    (-)-Penbutolol ((S)-Penbutolol) is a potent β-adrenoceptor and 5-HT receptor antagonist with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3.
    (-)-Penbutolol
  • HY-116594
    OPC-14523 free base
    		Agonist
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
    OPC-14523 free base
  • HY-118152
    Org-12962
    		Agonist 99.93%
    Org-12962 is a potent, selective and brain-penetrant and 5-HT2C receptor agonist with a pEC50 value of 7.01. Org-12962 also exhibits high effacy for the 5-HT2A and 5-HT2B receptor with pEC50s of 6.38 and 6.28, respectively.Org-12962 displays antiaversive effects in a rat model of panic-like anxiety.
    Org-12962
  • HY-12959
    Repinotan
    		Agonist
    Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.
    Repinotan
  • HY-112390
    Syk Inhibitor II dihydrochloride
    		Inhibitor
    Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect.
    Syk Inhibitor II dihydrochloride
  • HY-B0352B
    (R)-Mirtazapine
    		Antagonist 99.79%
    (R)-Mirtazapine ((R)-Org3770) is a R( )-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4.
    (R)-Mirtazapine
  • HY-14441
    ML 10302
    		Agonist 98.95%
    ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases.
    ML 10302
  • HY-103145
    PNU-22394 hydrochloride
    		Agonist 98.79%
    PNU-22394 hydrochloride is an agonist for 5-HT, with Ki of 6.1 and 10 nM, for 5-HT2C and 5-HT2A, respectively.
    PNU-22394 hydrochloride
  • HY-17038S2
    Agomelatine-d3
    		Antagonist 98.0%
    Agomelatine-d3 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.
    Agomelatine-d<sub>3</sub>
  • HY-B2089
    Cinitapride
    		Modulator 98.24%
    Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a 5-HT2 and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research.
    Cinitapride
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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