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-161246
    uPSEM792
    		Agonist 98.02%
    uPSEM792 is a pharmacologically selective effector molecules (PSEM) agonist for PSAM4-GlyR, with an affinity of Ki of 0.7 nM. uPSEM792 is a substrate for efflux transporters in brains of wild type and dual P-gp and BCRP knockout mice. uPSEM7952 is a possible lead for developing the PET radioligand for PSAM4-GlyR.
    uPSEM792
  • HY-W052508
    Norquetiapine
    		Modulator 99.95%
    Norquetiapine ( N-Desalkylauetiapine), a metabolite of Quetiapine (HY-14544), is a selective HCN1 channel inhibitor, with an IC50 of 13.9 μM. Norquetiapine 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 blocks the human cardiac sodium channel Nav1.5 in a state-dependent manner. Norquetiapine shows partial anti-inflammatory effects in LPS (HY-D1056) injected C57BL/6 mice. Norquetiapine can be used for the study of depression and inflammation.
    Norquetiapine
  • HY-118010A
    (+)-Norfenfluramine hydrochloride
    		Agonist 99.77%
    (+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease.
    (+)-Norfenfluramine hydrochloride
  • HY-122537A
    Arotinolol
    		Antagonist 99.93%
    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
  • HY-W131725
    (+)-Norfenfluramine
    		Agonist 98.79%
    (+)-Norfenfluramine a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine can be used for the research of primary pulmonary hypertension and valvular heart disease.
    (+)-Norfenfluramine
  • HY-113254
    13,14-Dihydro-15-keto-PGE2
    13,14-Dihydro-15-keto-PGE2 participates in Bifidobacterium animalis F1-7 to alleviate opioid-induced constipation by 5-HT pathway.
    13,14-Dihydro-15-keto-PGE2
  • HY-A0075
    Decloxizine dihydrochloride
    		Antagonist 99.69%
    Decloxizine (UCB-1402; NSC289116) dihydrochloride is an orally active bronchodilator that can penetrate the blood-brain barrier. Decloxizine dihydrochloride is a piperazine-type H1 histamine receptor antagonist. Decloxizine dihydrochloride selectively blocks H1 histamine receptors, inhibiting histamine-induced capillary dilation, edema, and itching. Decloxizine dihydrochloride has some 5-HT2 receptor antagonistic activity. Decloxizine dihydrochloride can be used in studies of urticaria, allergic rhinitis, and bronchial asthma.
    Decloxizine dihydrochloride
  • HY-B0731A
    Perospirone
    		Modulator 99.03%
    Perospirone (SM-9018 free base) is an orally active antagonist of 5-HT2A receptor (Ki=0.6 nM) and dopamine D2 receptor (Ki=1.4 nM), and also a partial agonist of 5-HT1A receptor (Ki=2.9 nM). Perospirone is an atypical antipsychotic agent and has the potential for schizophrenic disease research.
    Perospirone
  • HY-19469
    Roluperidone
    		99.86%
    Roluperidone (CYR-101) is a novel cyclic amide derivative that has high equipotent affinities for 5-HT2A and sigma-2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and sigma-2, respectively).
    Roluperidone
  • HY-N2510
    Myristicin
    		Antagonist 99.89%
    Myristicine is an orally bioavailable serotonin receptor antagonist and weak monoamine oxidase (MAO) inhibitor. Myristicine also exerts anti-cancer effects on gastric cancer cells by inhibiting the EGFR/ERK signaling pathway. Myristicine is the main component of nutmeg essential oil and has anti-cancer, anti-proliferative, antibacterial, anti-inflammatory and apoptosis-inducing effects. Myristicine abuse can produce hallucinogenic effects, organ damage, etc.
    Myristicin
  • HY-103101
    LP44 hydrochloride
    		Agonist 98.12%
    LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration.
    LP44 hydrochloride
  • HY-N0145R
    Puerarin (Standard)
    		Antagonist
    Puerarin (Standard) is the analytical standard of Puerarin. This product is intended for research and analytical applications. Puerarin, an isoflavone extracted from Radix puerariae, is a 5-HT2C receptor antagonist.
    Puerarin (Standard)
  • HY-32329A
    Setiptiline maleate
    		Antagonist 99.94%
    Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
    Setiptiline maleate
  • HY-17407
    Ziprasidone hydrochloride monohydrate
    		Antagonist 98.11%
    Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
    Ziprasidone hydrochloride monohydrate
  • HY-W028142
    Quipazine
    		Agonist
    Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research.
    Quipazine
  • HY-19818A
    NAN-190 hydrobromide
    		Antagonist 98.15%
    NAN-190 hydrobromide is a serotonin receptor 5-HT antagonist. NAN-190 is a selective antagonist of 5-HT1A.
    NAN-190 hydrobromide
  • HY-B0032
    Lurasidone Hydrochloride
    		Modulator 99.86%
    Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
    Lurasidone Hydrochloride
  • HY-101331
    Phenylbiguanide
    		Agonist 98.0%
    Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
    Phenylbiguanide
  • HY-18099
    S1RA
    		Antagonist 98.96%
    S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice.
    S1RA
  • HY-B0595
    Ramosetron Hydrochloride
    		Antagonist 99.96%
    Ramosetron (YM060 free base) Hydrochloride is an orally active 5-HT3 antagonist that improves dysphoria, interference with activity and food avoidance. Ramosetron Hydrochloride is promising for research of irritable bowel syndrome with diarrhea.
    Ramosetron Hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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