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-103140
    Ro60-0175 fumarate
    		Agonist 99.47%
    Ro60-0175 fumarate is a potent and selective agonist of 5-HT2C receptor.
    Ro60-0175 fumarate
  • HY-103154
    SB228357
    		Antagonist 99.43%
    SB228357 is a selective, potent and orall active 5-HT2C/2B receptor antagonist with pKi values of 6.9, 8.0 and 9.0 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. SB228357 has antidepressant/anxiolytic effects.
    SB228357
  • HY-14261S
    Vilazodone-d8
    		Inhibitor ≥99.0%
    Vilazodone-d8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist.
    Vilazodone-d<sub>8</sub>
  • HY-B0197
    Naratriptan
    		Agonist
    Naratriptan is an orally active and selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.
    Naratriptan
  • 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-19477
    SB-616234-A
    		Antagonist 98.14%
    SB-616234-A is a selective and orally bioavailable 5-HT1B receptor antagonist, with anxiolytic and antidepressant activity.
    SB-616234-A
  • 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-108057A
    Facinicline hydrochloride
    		Antagonist 99.66%
    Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM.
    Facinicline hydrochloride
  • 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-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-133113S
    7-Desmethyl-agomelatine-d3
    		≥99.0%
    7-Desmethyl-agomelatine-d3 is a deuterium labeled 7-Desmethyl-agomelatine. 7-Desmethyl-agomelatine is a metabolite of Agomelatine.
    7-Desmethyl-agomelatine-d<sub>3</sub>
  • 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-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-126057S
    (R)-Praziquantel-d11
    		Agonist 99.57%
    (R)-Praziquantel-d11 is the deuterium labeled (R)-Praziquantel. (R)-Praziquantel, the active enantiomer of Praziquantel, is a partial agonist of the human 5-HT2B receptor. (R)-Praziquantel acts as an antischistosomal eutomer.
    (R)-Praziquantel-d<sub>11</sub>
  • 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-103110
    ST1936
    		Agonist 99.70%
    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-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
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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