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-148038
    5-HT3 antagonist 5
    		Antagonist 99.75%
    5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice.
    5-HT3 antagonist 5
  • HY-W018475
    Rizatriptan
    		Agonist
    Rizatriptan (MK 462 free base) is an orally active 5-HT1B/5-HT1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache.
    Rizatriptan
  • HY-B0121A
    Sumatriptan hydrochloride
    		Agonist
    Sumatriptan hydrochloride (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan hydrochloride can be used for migraine headache research.
    Sumatriptan hydrochloride
  • HY-19668A
    SGS518 oxalate
    		Antagonist
    SGS518 oxalate is a selective 5-HT6R antagonist. SGS518 oxalate can be used for the research of cognitive impairments such as amnesia, anxiety and depression, and it is effective in protecting mouse retina at high doses[1]
    SGS518 oxalate
  • HY-21994
    Org-12962 hydrochloride
    		Agonist
    Org 12962 hydrochloride is a potent, selective and efficacious 5-HT2C receptor agonist and exhibits pEC50 values of 7.01, 6.38 and 6.28 for 5-HT2C, 5-HT2A and 5-HT2A, respectively. Org 12962 hydrochloride is effective in panic-like anxiety animal model.
    Org-12962 hydrochloride
  • HY-103144A
    WAY 629
    		Agonist
    WAY 629 is a potent and selective 5-HT2C agonist with EC50s of 426, 260000 nM for 5-HT2C and 5-HT2A, respectively. WAY 629 decreases feeding behavior.
    WAY 629
  • HY-106379
    Lurosetron
    		Antagonist
    Lurosetron (GR-87442) is a 6-fluoro analogue of Alosetron (HY-70050A). Lurosetron is a serotonin 5-HT3 receptor antagonist. Lurosetron inhibits recombinant (rbt) CYP1A2, with an IC50 of 0.1 μM. Lurosetron also inhibits other CYP isoforms, including rbtCYP2C9 and rbtCYP3A4 with IC50s ranging between 3.5 μM and 16 μM..
    Lurosetron
  • HY-W794785
    WAY 208466
    		Agonist
    WAY 208466 is a selective 5-HT6 receptor agonist with an EC50 of 7.3 nM. WAY-208466 increases GABA levels following both acute and chronic administration in the dorsolateral frontal cortex of rat models with stereotaxic surgery. WAY 208466 can be used for anxiety-related disorders like obsessive compulsive disorder (OCD) research.
    WAY 208466
  • HY-W744029
    Clothiapine-d8
    Clothiapine-d8 is the deuterium labeled Clothiapine (HY-117083). Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties.
    Clothiapine-d<sub>8</sub>
  • HY-B1059R
    Levosulpiride (Standard)
    		Antagonist
    Levosulpiride (Standard) is the analytical standard of Levosulpiride. This product is intended for research and analytical applications. Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class.
    Levosulpiride (Standard)
  • HY-169451
    Cannabidiolic acid methyl ester
    		Modulator
    Cannabidiolic acid methyl ester (HU-580) is an orally active cannabidiolic acid analogue. Cannabidiolic acid methyl ester can enhance the activation of 5-HT1A receptor and increase the expression of c-Fos and NeuN in specific hypothalamic nuclei of rats. Cannabidiolic acid methyl ester has anti-nausea, anti-anxiety and anti-injury effects.
    Cannabidiolic acid methyl ester
  • HY-14442
    ML 10302 hydrochloride
    		Agonist
    ML 10302 hydrochloride is a potent and selective 5-HT4 receptor agonist, with an EC50 of 4 nM. ML 10302 hydrochloride displays more than 680-fold selectivity over 5-HT3 receptor in binding assay.
    ML 10302 hydrochloride
  • HY-103090A
    NPS ALX Compound 4a dihydrochloride
    		Antagonist
    NPS ALX Compound 4a dihydrochloride is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM.
    NPS ALX Compound 4a dihydrochloride
  • HY-B1658B
    Frovatriptan succinate
    		Agonist
    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 succinate
  • HY-106943
    1192U90
    		Agonist
    1192U90 is an antipsychotic agent, dopamine D2 receptor antagonist as well as serotonin 5-HT1a receptor agonist. 1192U90 reduces the number of spontaneously firing neurons in the limbic dopamine system.
    1192U90
  • HY-118775
    LEK 8804
    		Agonist
    LEK 8804 is a compound with 5-HT1A receptor agonist and 5-HT2 receptor antagonist properties, and has the activity of modulating related receptor-mediated behavioral responses. LEK 8804 can induce spontaneous tail-flick response in rats in a dose-dependent manner, showing complete 5-HT1A agonist activity, and can inhibit 5-HTP-induced head twitch response in mice, probably through antagonism of 5-HT2 receptors rather than agonism of 5-HT1A receptors.
    LEK 8804
  • HY-B1101AR
    Pimethixene maleate (Standard)
    		Antagonist
    Pimethixene maleate (Standard) is the analytical standard of Pimethixene maleate. This product is intended for research and analytical applications. Pimethixene maleate is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene maleate is a highly potent antagonist of 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, histamine H1, dopamine D2 and D4.4 as well as muscarinic M1 and M2 receptors, with pKis of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
    Pimethixene maleate (Standard)
  • HY-175509
    5-HT2A agonist 6
    		Agonist
    5-HT2A agonist 6 (compound 2-6) is a 5-HT2A agonist with an EC50 of 1.7 nM. 5-HT2A agonist 6 is used in the study of stress-related disorders, namely depression, anxiety, and post-traumatic stress disorder.
    5-HT2A agonist 6
  • HY-156533A
    5-HT2 agonist-1 free base
    		Agonist
    5-HT2 agonist-1 (Compound 24) free base is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.
    5-HT2 agonist-1 free base
  • HY-A0274
    Ramosetron
    		Antagonist
    Ramosetron (YM060 free base) is an orally active 5-HT3 antagonist that improves dysphoria, interference with activity and food avoidance. Ramosetron is promising for research of irritable bowel syndrome with diarrhea.
    Ramosetron
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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