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-A0039
    Eletriptan
    		Agonist
    Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine.
    Eletriptan
  • HY-106578
    Quinupramine
    Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system[1][2].
    Quinupramine
  • HY-109543A
    Indisetron dihydrochloride
    		Antagonist
    Indisetron dihydrochloride is a 5-HT3 receptor antagonist with anti-emetic activity.
    Indisetron dihydrochloride
  • HY-171232
    Jimscaline
    		Agonist
    Jimscaline (compound R-(-)2) is a 5-HT2A agonist and mescaline analogue that can be utilized in neurological research.
    Jimscaline
  • HY-168443
    HTR2A antagonist 1
    		Antagonist
    HTR2A antagonist 1 (Compound 15f) is a HTR2A antagonist, with an IC50 of 42.79 nM. HTR2A antagonist 1 induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells via the activation of p53/p21/caspase 3 signaling. HTR2A antagonist 1 has good liver microsomal stability. HTR2A antagonist 1 can be used for the research of colorectal cancer.
    HTR2A antagonist 1
  • HY-14152
    Prucalopride hydrochloride
    		Agonist
    Prucalopride hydrochloride is an orally active, selective and specific 5-HT4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride hydrochloride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride hydrochloride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride hydrochloride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.
    Prucalopride hydrochloride
  • HY-W615853
    5-HT1A modulator 4
    		Ligand
    5-HT1A modulator 4 (Compound 1) is a ligand of 5-HT receptors. 5-HT1A modulator 4 has Ki values of 2.18 μM and 19.7 μM for 5-HT1A and 5-HT2A, respectively.
    5-HT1A modulator 4
  • HY-14431A
    Cerlapirdine hydrochloride
    		Antagonist
    Cerlapirdine hydrochloride is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine hydrochloride has the potential for researching the Alzheimer's disease.
    Cerlapirdine hydrochloride
  • HY-182701
    5-HT3 antagonist-7
    		Antagonist
    5-HT3 antagonist-7 (Compound 7e) is a competitive and selective 5-HT3 receptor antagonist. 5-HT3 antagonist-7 inhibits 5-HT-induced contractions in guinea pig ileum and guinea pig thoracic aorta. 5-HT3 antagonist-7 prevents 2-methyl-5-HT-induced vomiting episodes in ferrets.
    5-HT3 antagonist-7
  • HY-W040555
    Norquetiapine dihydrochloride
    		Modulator 99.91%
    Norquetiapine ( N-Desalkylauetiapine) dihydrochloride, a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine dihydrochloride selectively inhibits noradrenaline reuptake, is a partial 5-HT1A (Ki = 45 nM) receptor agonist, and acts as an antagonist at presynapticα2 (Ki = 237 nM), 5-HT2C(Ki = 107 nM), and 5-HT7 (Ki = 76 nM) receptors. Norquetiapine dihydrochloride blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine dihydrochloride shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine dihydrochloride can be used for the study of depression and inflammation.
    Norquetiapine dihydrochloride
  • HY-18596
    SB-215505
    		Antagonist 98.91%
    SB-215505 is an orally active and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively. SB-215505 increases wakefulness and motor activity in rats.
    SB-215505
  • HY-103404
    PNU-96415E
    		Antagonist
    PNU-96415E is a selective D4/5-HT2A antagonist. PNU-96415E may have potential antipsychotic efficacy.
    PNU-96415E
  • HY-174466
    5-HT2AR ligand 1
    		Ligand
    5-HT2AR ligand 1 (Compound 2 cis) is a 5-HT2AR ligand with nanomolar affinity for 5-HT2AR (Ki: 32 nM). 5-HT2AR ligand 1 is capable of inducing β-arrestin 2 recruitment. 5-HT2AR ligand 1 can be used in the research of neurological diseases.
    5-HT2AR ligand 1
  • HY-B1658BS
    Frovatriptan-d3 succinate
    		Agonist
    Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.
    Frovatriptan-d<sub>3</sub> succinate
  • HY-165624A
    (S)-LY-41
    		Agonist
    (S)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (S)-LY-41 is a potent and selective 5-HT1A receptor agonist. (S)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (S)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (S)-LY-41 can induce the 5-HT behavioral syndrome. (S)-LY-41can be used for the research of neurological disease, such as depression and anxiety.
    (S)-LY-41
  • HY-12560
    PNU-282987 free base
    		Antagonist
    PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems.
    PNU-282987 free base
  • HY-B1658S
    Frovatriptan-d3 hydrochloride
    Frovatriptan-d3 (hydrochloride) is the deuterium labeled Frovatriptan. Frovatriptan is a potent 5-HT1B//D receptor agonist and has the highest 5-HT1B potency in the triptan class. Frovatriptan is apparently cerebroselective. Frovatriptan is efficacious and even superior in some endpoints also when taken during the headache phase in migraine attacks with aura.
    Frovatriptan-d<sub>3</sub> hydrochloride
  • HY-175285
    5-HT2AR-IN-1
    		Inhibitor
    5-HT2AR-IN-1 (Compound Ie) is an orally active 5-hydroxytryptamine 2A receptor (5-HT2AR) inhibitor with antidepressant efficacy. 5-HT2AR-IN-1 reduces 5-HT2AR expression and SERT protein levels. 5-HT2AR-IN-1 is promising for research of central nervous system (CNS), such as depression and addiction-related disorders.
    5-HT2AR-IN-1
  • HY-A0175
    Butriptyline
    		Inhibitor
    Butriptyline (Butriptylene) is an orally active tricyclic antidepressant that slightly enhances central 5-HT effects. Butriptyline does not inhibit brain norepinephrine uptake. Butriptyline can be used for depression research.
    Butriptyline
  • HY-105277
    Amesergide
    		Antagonist
    Amesergide is a serotonin (5-HT1C/2) antagonist. Amesergide can result in a reduction of progeny body weight gains in maternal animals. Amesergide can be studied in research on depression.
    Amesergide
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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