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-100243
    (+)-Norcisapride
    Modulator 99.32%
    (+)-Norcisapride (Ticalopride) is a potent 5-HT4 agonist and a 5-HT3 antagonist. (+)-Norcisapride has activity in animals models of constipation.
    (+)-Norcisapride
  • HY-105201
    Fabesetron
    Antagonist
    Fabesetron (FK1052) is an orally active 5-HT3 receptor antagonist with 5-HT4 receptor antagonistic activity. Fabesetron (FK1052) can be used in the study for both acute and delayed emesis induced by cancer chemotherapy.
    Fabesetron
  • 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-W741575
    Iloperidone carboxylic acid
    Ligand 99.6%
    Iloperidone carboxylic acid (P95-12113) is the metabolite of Iloperidone (HY-17410). Iloperidone carboxylic acid exhibits good affinity for 5-HT2A receptor with pKi of 8.15, and moderate affinity for adrenergic receptor α1/α2B/α2C.
    Iloperidone carboxylic acid
  • HY-107613A
    R 59-022 hydrochloride
    Antagonist 98.88%
    R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
    R 59-022 hydrochloride
  • HY-N1745
    2'-O-Methylisoliquiritigenin
    Activator 99.06%
    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-B0750B
    Dolasetron Mesylate hydrate
    Antagonist 99.88%
    Dolasetron Mesylate hydrate (MDL-73147EF hydrate) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
    Dolasetron Mesylate hydrate
  • HY-139201E
    Poly-D-lysine hydrobromide (MW 150000-300000)
    Activator
    Poly-D-lysine hydrobromide (MW 150000-300000) is a synthetic polymer composed of D-lysine residues and is one of the most widely used matrices in neural cell culture applications. Poly-D-lysine hydrobromide (MW 150000-300000) can be used as a non-specific cell adhesion enhancer. Poly-D-lysine hydrobromide (MW 30000-70000) is an orally active CaSR agonist peptide that indirectly activates the 5-HT₃ receptor signaling pathway, delaying gastric emptying and thereby slowing the rate at which glucose enters the small intestine and is absorbed.
    Poly-D-lysine hydrobromide (MW 150000-300000)
  • 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-N9141
    Nantenine
    Antagonist 98%
    Nantenine is a serotonergic receptor antagonist. Nantenine selectively inhibits the contractile response of tissues to serotonin. Nantenine can be isolated from Nandina domestica.
    Nantenine
  • HY-19134
    EMD 56551
    Agonist
    EMD 56551 is a potent and selective 5-HT1A receptor agonist. EMD 56551 exerts anxiolytic activity.
    EMD 56551
  • HY-B0407AR
    Chlorpromazine hydrochloride (Standard)
    Antagonist
    Chlorpromazine (hydrochloride) (Standard) is the analytical standard of Chlorpromazine (hydrochloride). This product is intended for research and analytical applications. Chlorpromazine hydrochloride is an orally active, blood-brain barrier-transparent antipsychotic agent that effectively antagonises D2 dopamine receptors and 5-HT2A, which is widely used in schizophrenia and other psychiatric disorders. Chlorpromazine hydrochloride exerts anti-cancer activity through a variety of pathways, including anti-proliferation, induction of autophagy and cycle arrest (G2-M phase), inhibition of cytochrome c oxidase (CcO), inhibition of tumour growth and metastasis, and inhibition of tumour immune escape. Chlorpromazine hydrochloride also blocks hNav1.7 channels (IC50=25.9 μM; concentration-dependent) and HERG potassium channels (IC50=21.6 μM), which has potential for analgesic and cardiac arrhythmic studies. Chlorpromazine hydrochloride also can inhibit clathrin-mediated endocytosis.
    Chlorpromazine hydrochloride (Standard)
  • 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-129101
    (-)-Eseroline fumarate
    Antagonist 98.03%
    (-)-Eseroline fumarate is a metabolic of Physostigmine (HY-N6608), an AChE inhibitor. (-)-Eseroline fumarate elicits a leakage of lactic acid dehydrogenase (LDH) from cancer cells. (-)-Eseroline fumarate also induces the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, thus induce cell death. (-)-Eseroline fumarate inhibits the electrically evoked twitches of the mouse vas deferens and of the guinea-pig ileum.
    (-)-Eseroline fumarate
  • 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
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