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-110001
    (S)-WAY 100135 dihydrochloride
    		Antagonist 99.9%
    (S)-WAY 100135 dihydrochloride is a highly selective and potent antagonist of 5-HT 1A (IC50=33.9 nM). (S)-WAY 100135 dihydrochloride has anxiolytic activity in animal models.
    (S)-WAY 100135 dihydrochloride
  • HY-164703
    Lumateperone metabolite 1
    		Control 98.26%
    Lumateperone metabolite 1 (Formula T) is a metabolite of Lumateperone (HY-17637). Lumateperone (ITI-007) is an orally active 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator
    Lumateperone metabolite 1
  • HY-101609
    Lesopitron dihydrochloride
    		Agonist 98.0%
    Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes.
    Lesopitron dihydrochloride
  • HY-101755
    Tedatioxetine hydrobromide
    		Antagonist 99.83%
    Tedatioxetine (Lu AA24530) hydrobromide acts as a serotonin and norepinephrine (NE)-preferring triple reuptake inhibitor (TRI) and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist. ,
    Tedatioxetine hydrobromide
  • HY-101815
    Lidanserin
    		Antagonist ≥98.0%
    Lidanserin (ZK-33839) acts as a 5-HT2A and α1-adrenergic receptor antagonist.
    Lidanserin
  • HY-14848
    Naluzotan
    		Agonist 98.05%
    Naluzotan is a novel, potent, and selective amidosulfonamide 5-HT1A agonist with IC50 and Ki of appr 20 nM and 5.1 nM, used for the treatment of anxiety and depression; Also a weak hERG K+ channel blocker, with IC50 of 3800 nM.
    Naluzotan
  • HY-19110
    RG-12915
    		Antagonist
    RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
    RG-12915
  • HY-161511
    LPH-5
    		Antagonist 98.08%
    LPH-5 is a selective 5-HT2A receptor agonist (EC50=190 nM). LPH-5 works by selectively activating the 5-HT2A receptor, which may be involved in regulating mood, perception, and other central nervous system functions associated with the 5-HT2A receptor. LPH-5 can be used to further explore the 5-HT2A receptor in psychiatric disorders, including depression, anxiety, and substance abuse disorders.
    LPH-5
  • HY-100552
    VUF10166
    		Antagonist 99.83%
    VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM.
    VUF10166
  • HY-B1495
    Quipazine maleate
    		Agonist 98.0%
    Quipazine maleate is a 5-HT agonist that causes behavioural changes such as hyperactivity. Quipazine maleate also shows a weak reversible MAO inhibitory activity.
    Quipazine maleate
  • HY-16729A
    Relenopride hydrochloride
    		Agonist 99.85%
    Relenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility.
    Relenopride hydrochloride
  • HY-12709
    ARC 239
    		Inhibitor 99.71%
    ARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM.
    ARC 239
  • HY-156532
    5-HT2C agonist-3
    		Agonist 99.86%
    5-HT2C agonist-3 ((+)-19) is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 has antipsychotic drug-like activity. 5-HT2C agonist-3 blocks Amphetamine-induced hyperactivity.
    5-HT2C agonist-3
  • HY-B0121BS
    Sumatriptan-d6 succinate
    		Agonist 99.63%
    Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research.
    Sumatriptan-d<sub>6</sub> succinate
  • HY-106584
    Mosapramine
    		Antagonist 98.58%
    Mosapramine (Clospipramine) is an orally active antipsychotic agent and one of the metabolites of Clocapramine (HY-B2073) after oral absorption. Mosapramine exerts its effects by specifically binding to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, with a D2/5-HT2 receptor occupancy ratio of 7.4. Mosapramine induces typical neuropharmacological responses in rat brain regions, including extrapyramidal symptoms, hyperprolactinemia, increased salivation, constipation, and upregulated Fos protein expression. Mosapramine also features a reduced incidence of weight loss. Mosapramine is applicable to research related to schizophrenia.
    Mosapramine
  • HY-103110
    ST1936
    		Agonist 98.66%
    ST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
    ST1936
  • HY-100971
    Spiramide
    		Antagonist 99.23%
    Spiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity.
    Spiramide
  • HY-B0352A
    (S)-Mirtazapine
    		Antagonist 99.76%
    (S)-Mirtazapine ((S)-Org3770) is a S(+)-enantiomer of Mirtazapine with pronociceptive properties in an animal model of acute thermal nociception. (S)-Mirtazapine is a stereoselective 5-HT2 receptor antagonist. (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2.
    (S)-Mirtazapine
  • HY-15856
    cis-(Z)-Flupentixol dihydrochloride
    		Antagonist
    cis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with Ki values of 0.38 nM and 7 nM for D2 receptor and 5-HT2A, respectively.
    cis-(Z)-Flupentixol dihydrochloride
  • HY-14431
    Cerlapirdine
    		Antagonist 98.84%
    Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.
    Cerlapirdine
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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