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

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-111419
    DSP-1053
    Agonist 99.75%
    DSP-1053, a benzylpiperidine derivative, is a potent Serotonin Transporter (SERT) inhibitor with a Ki of 1.02 nM. DSP-1053 shows partial 5-HT1A receptor agonistic activity with a Ki of 5.05 nM. DSP-1053 has antidepressant activity.
    DSP-1053
  • HY-116565A
    Usmarapride free base
    Agonist 99.91%
    Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.
    Usmarapride free base
  • HY-14546S1
    Aripiprazole-d8
    Agonist 99.86%
    Aripiprazole (1,1,2,2,3,3,4,4-d8) is the deuterium labeled Aripiprazole. Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
    Aripiprazole-d<sub>8</sub>
  • HY-19946
    Eptapirone
    Agonist 99.91%
    Eptapirone (F11440) is a potent, selective and orally active 5-HT1A receptor agonist (pKi = 8.33). Eptapirone can inhibit cAMP production. Eptapirone can reduce 5-HT levels and increase corticosterone levels. Eptapirone shows potent anxiolytic and antidepressant potential. Eptapirone can be used for the research of neurological disease, such as anxiety and depression.
    Eptapirone
  • HY-14848A
    Naluzotan hydrochloride
    Agonist 99.63%
    Naluzotan hydrochloride 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 hydrochloride
  • HY-14547A
    Bifeprunox mesylate
    Agonist 99.89%
    Bifeprunox mesylate is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox mesylate is an antipsychotic for the research of schizophrenia.
    Bifeprunox mesylate
  • HY-19650
    Pumosetrag Hydrochloride
    Agonist 99.77%
    Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
    Pumosetrag Hydrochloride
  • HY-137572
    (R)-DOI hydrochloride
    Agonist 99.63%
    (R)-DOI hydrochloride is a selective 5HT2A receptor agonist. (R)-DOI hydrochloride has anti-inflammatory, anti-oxidative stress, and lysosomal function-improving effects. (R)-DOI hydrochloride can be used for the researches of inflammation and neurological disease, such as Alzheimer's disease.
    (R)-DOI hydrochloride
  • HY-14785A
    Befiradol hydrochloride
    Agonist 99.93%
    Befiradol (NLX-112) hydrochloride is a highly selective 5-HT1A receptor agonist that acts on both presynaptic and postsynaptic sites. Befiradol hydrochloride attenuates fentanyl-induced respiratory depression in neonatal and adult rats. Befiradol reduces the duration of fentanyl-induced analgesia and sedation in adult rats. Befiradol hydrochloride can be used in studies related to opioid-induced respiratory depression.
    Befiradol hydrochloride
  • HY-160921
    Capeserod
    Agonist 98.66%
    Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a Ki of 0.6 nM for 5-HT4 receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models.
    Capeserod
  • HY-15394S1
    (Rac)-Rotigotine-d3 hydrochloride
    Agonist
    (Rac)-Rotigotine-d3 hydrochloride is a deuterium labeled (Rac)-Rotigotine (hydrochloride) (HY-15394). (Rac)-Rotigotine hydrochloride is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    (Rac)-Rotigotine-d<sub>3</sub> hydrochloride
  • HY-160887
    FPT
    Agonist 98.06%
    FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models.
    FPT
  • HY-103105A
    LP 12 hydrochloride hydrate
    Agonist 99.0%
    LP 12 hydrochloride hydrate is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride hydrate displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively).
    LP 12 hydrochloride hydrate
  • HY-19134
    EMD 56551
    Agonist
    EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity.
    EMD 56551
  • HY-102057
    Felcisetrag
    Agonist 99.94%
    Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
    Felcisetrag
  • HY-B0716S1
    Urapidil-d3
    Agonist 99.93%
    Urapidil-d3 is the deuterium labeled Urapidil. Urapidil is an α1 adrenoreceptor antagonist and a 5-HT1A receptor agonist.
    Urapidil-d<sub>3</sub>
  • HY-W417914
    4-Methylamphetamine hydrochloride
    Agonist 99.86%
    4-Methylamphetamine hydrochloride is a 5-HT1A receptor agonist that induces hypothermia in rats by binding to the 5-HT1A receptor. Additionally, 4-Methylamphetamine hydrochloride acts on norepinephrine (NE), dopamine (DA), and serotonin (5-HT) transporters to increase the extracellular levels of these neurotransmitters. 4-Methylamphetamine hydrochloride can be used in the study of neurological disorders.
    4-Methylamphetamine hydrochloride
  • 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-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-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
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