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

PDF 7.25 MB

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-139233
    25P-NBOMe hydrochloride
    		Agonist
    25P-NBOMe hydrochloride is structurally categorized as a phenethylamine. 25P-NBOMe hydrochloride binds 5-HT receptors 5-HT2A and 5-HT2C with similar affinities.
    25P-NBOMe hydrochloride
  • HY-10564S1
    Sarpogrelate-d4 hydrochloride
    		Antagonist
    Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
    Sarpogrelate-d<sub>4</sub> hydrochloride
  • HY-19733S
    Lumateperone-CHC,d3 tosylate
    		Antagonist
    Lumateperone-13C,d3 (ITI-007-13C,d3) tosylate is 13C and deuterium labeled Lumateperone (tosylate). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
    Lumateperone-</sup>CH<sub>C,d<sub>3</sub> tosylate
  • HY-B0032AR
    Lurasidone (Standard)
    		Modulator
    Lurasidone (Standard) is the analytical standard of Lurasidone. This product is intended for research and analytical applications. Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
    Lurasidone (Standard)
  • HY-106124
    IS-159
    		Agonist
    IS-159 is a potent serotonin 5-HT1 agonist. IS-159 has the potential for the research of migraine.
    IS-159
  • HY-W653969
    Arotinolol-d5 hydrochloride
    		Antagonist
    Arotinolol-d5 (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
    Arotinolol-d<sub>5</sub> hydrochloride
  • HY-B0602B
    Desvenlafaxine fumarate
    		Inhibitor
    Desvenlafaxine (O-Desmethylvenlafaxine) fumarate is a selective serotonin and norepinephrine reuptake inhibitor. Desvenlafaxine (O-Desmethylvenlafaxine) fumarate is the major metabolite of the antidepressant venlafaxine. Desvenlafaxine (O-Desmethylvenlafaxine) fumarate has the potential for the research of depression and related disorders and diseases (extracted from patent WO2009049354A1).
    Desvenlafaxine fumarate
  • HY-105109
    Cilansetron
    		Antagonist
    Cilansetron is a 5-HT3 receptor antagonist. Cilansetron can be used in studies of irritable bowel syndrome.
    Cilansetron
  • HY-B1396R
    Nefazodone (hydrochloride) (Standard)
    		Antagonist
    Nefazodone (hydrochloride) (Standard) is the analytical standard of Nefazodone (hydrochloride). This product is intended for research and analytical applications. Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.
    Nefazodone (hydrochloride) (Standard)
  • HY-14541S2
    Olanzapine-d8
    		Antagonist
    Olanzapine-d8 is a deuterated labeled Olanzapine. 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-d<sub>8</sub>
  • HY-168747
    4-Bromo-2,5-DMMA
    		Ligand
    4-Bromo-2,5-DMMA (Compound 2) has affinity for 5-HT2 binding sites. 4-Bromo-2,5-DMMA has an ED50 of 0.82 mg/kg in the rat discrimination tests.
    4-Bromo-2,5-DMMA
  • HY-116603
    SB-236057
    SB-236057 is an inverse agonist of the 5-HT1B receptor that exhibits strong skeletal teratogenicity in rodents and rabbits. SB-236057 affects gene expression during embryonic development through interference with the Notch signaling pathway and interaction with r-esp1. SB-236057 induces somatic patterning and tail extension defects in rat embryos during early organogenesis.
    SB-236057
  • HY-14557R
    Pimavanserin (Standard)
    		Inhibitor
    Pimavanserin (Standard) is the analytical standard of Pimavanserin. This product is intended for research and analytical applications. Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
    Pimavanserin (Standard)
  • HY-10560R
    Temanogrel (Standard)
    		Antagonist
    Temanogrel (Standard) is the analytical standard of Temanogrel. This product is intended for research and analytical applications. Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.
    Temanogrel (Standard)
  • HY-70050B
    Alosetron ((Z)-2-butenedioate)
    		Antagonist
    Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z)-2-butenedioate is used for the research of irritable bowel syndrome (IBS). Alosetron (Z)-2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z)-2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects.
    Alosetron ((Z)-2-butenedioate)
  • HY-167639
    (S)-Ramosetron
    		Antagonist
    (S)-Ramosetron ((S)-YM060 (free base)) is an orally active antagonist of the 5-hydroxytryptamine 5-HT3 receptor. (S)-Ramosetron is promising for research of diseases related to nausea and vomiting, irritable bowel syndrome (IBS).
    (S)-Ramosetron
  • HY-123498
    MCI-225 (dehydratase)
    		Antagonist
    MCI-225 dehydratase is an orally active and selective noradrenaline reuptake inhibitor. MCI-225 dehydratase also is a 5-HT3 antagonist and shows antidepressant effects in vivo.
    MCI-225 (dehydratase)
  • HY-106807
    Litoxetine
    		Inhibitor
    Litoxetine (SL 81.0385) is a selective 5-HT uptake inhibitor. Litoxetine is a 5-HT3 receptor antagonist with a Ki of 85 nM for cerebral 5-HT3 receptors. Litoxetine is an antidepressant and has antiemetic properties.
    Litoxetine
  • HY-103153R
    SB 204741 (Standard)
    		Antagonist
    SB 204741 (Standard) is the analytical standard of SB 204741. This product is intended for research and analytical applications. SB 204741 is a selective and high affinity 5-HT2B antagonist with a pKi value of 7.1.
    SB 204741 (Standard)
  • HY-169140
    Zalospirone
    		Agonist
    Zalospirone (WY-47846) is a novel cyclic imide with 5-HT1A partial agonist activity. Zalospirone shows antidepressant efficacy.
    Zalospirone
Cat. No. Product Name / Synonyms Application Reactivity