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-103094R
    LY266097 hydrochloride (Standard)
    		Inhibitor
    LY266097 hydrochloride (Standard) is the analytical standard of LY266097 hydrochloride (HY-103094). This product is intended for research and analytical applications. LY266097 hydrochloride is a selective 5-HT2B receptor antagonist with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, 5-HT2C, respectively. 5-HT2B receptor blockade contributes to the research in depression.
    LY266097 hydrochloride (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-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 99.98%
    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-121653R
    Flesinoxan (Standard)
    		Agonist
    Flesinoxan (Standard) is the analytical standard of Flesinoxan. This product is intended for research and analytical applications. Flesinoxan is a hypotensive agent and a potent, high affinity and selective 5-hydroxytryptamine1A (5-HT1A) receptor agonist with an EC50 value of 24 nM. Flesinoxan also has effective anxiolytic/antidepressant effects.
    Flesinoxan (Standard)
  • 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-B1213S
    Trimipramine-d3 maleate
    		Antagonist
    Trimipramine-d3 (maleate) is the deuterium labeled Trimipramine maleate. Trimipramine maleate is a 5-HT receptor antagonist, with pKis of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively.
    Trimipramine-d<sub>3</sub> maleate
  • 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-B1371R
    Spiperone (Standard)
    		Antagonist
    Spiperone (Standard) is the analytical standard of Spiperone. This product is intended for research and analytical applications. Spiperone (Spiroperidol) is a potent dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist. Spiperone is also a labelled ligand for neuroleptic receptors. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. Spiperone has the potential for the research of neurology diseases.
    Spiperone (Standard)
  • HY-101105AR
    SB-224289 hydrochloride (Standard)
    		Antagonist
    SB-224289 (hydrochloride) (Standard) is the analytical standard of SB-224289 (hydrochloride) (HY-101105A). This product is intended for research and analytical applications. SB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
    SB-224289 hydrochloride (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-112061R
    8-OH-DPAT (Standard)
    		Agonist
    8-OH-DPAT (Standard) is the analytical standard of 8-OH-DPAT. This product is intended for research and analytical applications. 8-OH-DPAT is a potent and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
    8-OH-DPAT (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-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-105896R
    SB399885 (Standard)
    		Antagonist
    SB399885 (Standard) is the analytical standard of SB399885 (HY-105896). This product is intended for research and analytical applications. SB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pKi values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties.
    SB399885 (Standard)
  • 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-14604R
    Xaliproden hydrochloride (Standard)
    		Agonist
    Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.
    Xaliproden hydrochloride (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
5-HT Receptor Isoform Comparison

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