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-18137
    PF-04995274
    Agonist 99.95%
    PF-04995274 is a potent, high-affinity, orally active and partial serotonin 4 receptor (5-HT4R) agonist. PF-04995274 has an EC50 range of 0.26-0.47 nM for human 5-HT4A/4B/4D/4E (Ki range of 0.15-0.46 nM), and has an EC50 range of 0.59-0.65 nM for rat 5-HT4S/4L/4E (Ki of 0.30 nM for rat 5-HT4S). PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease.
    PF-04995274
  • HY-133113
    7-Desmethyl-agomelatine
    Antagonist 99.89%
    7-Desmethyl-agomelatine is a metabolite of Agomelatine. Agomelatineis a potent agonist at melatonin receptors (MT1 and MT2), and also is an antagonist of 5-HT2C.
    7-Desmethyl-agomelatine
  • HY-14541R
    Olanzapine (Standard)
    Antagonist
    Olanzapine (Standard) is the analytical standard of Olanzapine. This product is intended for research and analytical applications. Olanzapine (LY170053) is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine (Standard)
  • HY-N1745
    2'-O-Methylisoliquiritigenin
    Activator 98.44%
    2'-O-Methylisoliquiritigenin, isolated from the Arachis species, up-regulates 5-HT, NE, DA and GABA pathways, but does not put a very significant effect on ne NE pathway.
    2'-O-Methylisoliquiritigenin
  • 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-N7514
    Strictosidinic acid
    Inhibitor
    Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice.
    Strictosidinic acid
  • HY-19496
    4-Butyl-alpha-agarofuran
    ≥98.0%
    4-Butyl-alpha-agarofuran (AF 5) is an anxiolytic and antidepressant agent. 4-Butyl-alpha-agarofuran a α-agarofuran derivative that can be isolated from Gharu-wood. 4-Butyl-alpha-agarofuran can be used for the research of neurological disease research.
    4-Butyl-alpha-agarofuran
  • HY-19134
    EMD 56551
    Agonist
    EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity.
    EMD 56551
  • HY-141422A
    4,4-Diphenylbutylamine hydrochloride
    Antagonist 99.00%
    4,4-Diphenylbutylamine shows affinity for the 5-HT2A and H1 receptors with Kis of 2589 and 1670 nM, respectively.
    4,4-Diphenylbutylamine hydrochloride
  • 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-14559
    PRX-07034 hydrochloride
    Antagonist 98.97%
    PRX-07034 hydrochloride is a highly selective and potent 5-HT6 receptor antagonist with a Ki= 4-8 nM and an IC50 of 19 nM. PRX-07034 can be used for the research of enhancing working memory and cognitive flexibility.
    PRX-07034 hydrochloride
  • 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-100290
    5-HT1A modulator 1
    Modulator
    5-HT1A modulator 1 displays very high affinities for the 5HT1A, adrenergic α1 and dopamine D2 receptor with IC50s of 2 ±0.3 nM, 10 ± 3 nM and 40 ±9 nM, respectively.
    5-HT1A modulator 1
  • HY-169229
    GM-60186
    Inhibitor
    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-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 99.92%
    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-103112
    SB 243213 hydrochloride
    Antagonist
    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-153091
    BMY 14802
    Activator 98.96%
    BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM.
    BMY 14802
  • 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
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