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

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

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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-13527
    LY310762
    		Antagonist 98.89%
    LY310762 is a selective 5-HT1D receptor antagonist (Ki=249 nM) with a weak affinity for 5-HT1B receptor. LY310762 effectively abolishes the renal vasodilatory effects of 5-HT
    LY310762
  • HY-14264
    Cyamemazine
    		Antagonist 99.47%
    Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.
    Cyamemazine
  • HY-B1737
    Pirenperone
    		Antagonist 98.97%
    Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity.
    Pirenperone
  • HY-16687A
    Eltoprazine hydrochloride
    		Modulator 99.25%
    Eltoprazine (DU 28853) hydrochloride is a 5-HT1A/5-HT1B receptors agonist and a 5-HT2C receptor antagonist. Eltoprazine hydrochloride shows antiaggressive and anxiogenic effects.
    Eltoprazine hydrochloride
  • HY-169229
    GM-60186
    		Inhibitor 99.34%
    GM-60186 is a 5-HT receptor 2B (HTR2B) inhibitor with an IC50 of 257 nM. GM-60186 significantly inhibits colorectal cancer proliferation and migration.
    GM-60186
  • HY-105896
    SB399885
    		Antagonist 98.85%
    SB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pKi values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties.
    SB399885
  • HY-134807
    Indophagolin
    		Antagonist 98.05%
    Indophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.
    Indophagolin
  • HY-121653
    Flesinoxan
    		Agonist 99.88%
    Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects.
    Flesinoxan
  • HY-12706
    Spiroxatrine
    		Antagonist 99.25%
    Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect.
    Spiroxatrine
  • HY-59201A
    A-582941 dihydrochloride
    		Agonist 99.78%
    A-582941 dihydrochloride is a selective, orally active, blood-brain barrier-permeable α7 nAChR agonist, with Ki values of 10.8 nM and 17 nM in rat brain and human frontal cortex, respectively. A-582941 dihydrochloride exhibits agonistic activity at 5-HT3 receptors, with a Ki of 150 nM. A-582941 dihydrochloride triggers phosphorylation of ERK1/2 and CREB, inhibits GSK-3β via Ser-9 phosphorylation, increases acetylcholine release, induces the expression of Arc and c-Fos, activates brain regions associated with working memory and attention, and reduces cell death caused by nerve growth factor (NGF) deprivation. A-582941 dihydrochloride is applicable for the research of Alzheimer's disease and schizophrenia.
    A-582941 dihydrochloride
  • HY-16688A
    RU 24969 succinate
    		Agonist 99.58%
    RU 24969 succinate is a 5-HT receptor agonist with Ki values of 0.38 and 2.5 nM for 5-HT1B and 5-HT1A, respectively. RU 24969 decreases fluid consumption and increases forward locomotion. RU 24969 succinate can be used for the research of neurological disease.
    RU 24969 succinate
  • HY-B0002BS
    Ondansetron-d5
    		Antagonist 99.95%
    Ondansetron-d5 is the deuterium labeled Ondansetron (HY-B0002B). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy.
    Ondansetron-d<sub>5</sub>
  • HY-124821
    VA012
    		Modulator 99.34%
    VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin 5-HT2C receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research.
    VA012
  • HY-10457A
    Velusetrag hydrochloride
    		Agonist 98.95%
    Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease.
    Velusetrag hydrochloride
  • HY-14546S
    Aripiprazole-d8
    		Agonist 98.35%
    Aripiprazole-d8 (OPC-14597-d8) is the deuterium labeled Aripiprazole (HY-14546). 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-d<sub>8</sub>
  • HY-B0383
    Almotriptan malate
    		Agonist 99.53%
    Almotriptan malate (PNU180638) is an orally active, highly selective agonist of the 5-HT1B/1D receptor (5-HT1B/1D receptor), with EC50 values of 1.6 nM and 3.1 nM, respectively. Almotriptan malate shows moderate affinity for the 5-HT1F receptor, and weak affinity for the 5-HT1A, 5-HT6 and 5-HT7 receptors. Almotriptan malate induces intracranial vasoconstriction, inhibits nociceptive neurotransmission in the trigeminocervical complex, and suppresses the release of vasoactive peptides from trigeminal nerve endings. Almotriptan malate can be used in research related to migraine.
    Almotriptan malate
  • HY-117046A
    AVN-101 hydrochloride
    		Antagonist 99.59%
    AVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
    AVN-101 hydrochloride
  • HY-W344044
    Levomepromazine maleate
    		Antagonist 99.92%
    Levomepromazine maleate (Methotrimeprazine maleate) is an N-substituted phenylthiazine antipsychotic sedative that blocks multiple receptors. Levomepromazine maleate is a potent inhibitor of CYP2D6 and is useful in the study of schizophreni.
    Levomepromazine maleate
  • HY-103428
    LE 300
    		Antagonist 98.5%
    LE 300 is a potent and selective dopamine D1-like receptor antagonist with Kis of 1.9 nM and 7.5 nM in CHO cell membranes expressing human dopamine D1 and D5 receptors, respectively. LE 300 is an antagonist of the 5-HT2A receptor with a pA2 of 8.32 in a rat tail artery assay.
    LE 300
  • HY-103136
    R-96544
    		Antagonist 99.50%
    R-96544 is an orally active 5-HT2A receptor antagonist. R-96544 can inhibit platelet aggregation in vitro.
    R-96544
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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