1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

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-14542B
    Ziprasidone mesylate trihydrate
    Antagonist
    Ziprasidone (CP-88059) mesylate trihydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone mesylate trihydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
    Ziprasidone mesylate trihydrate
  • HY-136109A
    SEP-363856
    Agonist
    SEP-363856 (SEP-856), an orally active TAAR1 and 5-HT1A agonist and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 (SEP-856) has the potential for the study of schizophrenia.
    SEP-363856
  • HY-B2073
    Clocapramine
    Antagonist
    Clocapramine is an antagonist of the D2, 5-HT2A receptors.
    Clocapramine
  • HY-B0031S4
    Quetiapine hemifumarate-d8
    99.35%
    Quetiapine (hemifumarate)-d8 is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
    Quetiapine hemifumarate-d<sub>8</sub>
  • HY-15414AS
    Vortioxetine-d8 hydrobromide
    Inhibitor 99.41%
    Vortioxetine-d8 (Lu AA 21004-d8) hydrobromide is the deuterated form of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
    Vortioxetine-d<sub>8</sub> hydrobromide
  • HY-B0197AS
    Naratriptan-d3 hydrochloride
    Agonist
    Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan hydrochloride (HY-B0197A). Naratriptan hydrochloride is a selective 5-HT1B/1D receptor agonist. Naratriptan hydrochloride is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan hydrochloride also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan hydrochloride is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.
    Naratriptan-d<sub>3</sub> hydrochloride
  • HY-B1059S
    Levosulpiride-d3
    Antagonist 99.79%
    Levosulpiride-d3 is the deuterium labeled Levosulpiride. 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-d<sub>3</sub>
  • HY-13575A
    Blonanserin dihydrochloride
    Antagonist
    Blonanserin dihydrochloride is a potent and orally active 5-HT2A and dopamine D2 receptor antagonist, with Ki values of 0.812 and 0.142 nM, respectively. Blonanserin dihydrochloride is usually acts as an atypical antipsychotic agent, and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
    Blonanserin dihydrochloride
  • HY-136109B
    (Rac)-SEP-363856
    Agonist
    (Rac)-SEP-363856 is the racemate of SEP-363856. SEP-363856(SEP-856), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 (SEP-856) has the potential for the treatment of schizophrenia.
    (Rac)-SEP-363856
  • HY-162423
    CYB210010
    Agonist
    CYB210010 is an orally bioavailable, long-acting serotonin 5-HT2 receptor agonist that selectively targets 5-HT2A and 5-HT2C receptors (EC50: 4.1 n, 7.3 nM). CYB210010 can enter the central nervous system, cause a head twitch response (HTR), and is not prone to behavioral tolerance during chronic administration.
    CYB210010
  • HY-B2065
    Scopolamine hydrochloride
    Antagonist
    Scopolamine (Hyoscine) hydrochloride is a high-affinity muscarinic antagonist that can cross the blood-brain barrier. Scopolamine hydrochloride competitively antagonizes 5-HT3 receptors with an IC50 of 2.09 μM. Scopolamine hydrochloride can induce cognitive and memory deficits in animals. Scopolamine hydrochloride can be used in the research of preventing postoperative nausea and vomiting, motion sickness, nervous system diseases, etc.
    Scopolamine hydrochloride
  • HY-103107A
    LY334370 hydrochloride
    Agonist
    LY334370 hydrochloride is a selective 5-HT1F receptor agonist with a Kd value of 0.446 nM. LY334370 hydrochlorid has anti-migraine activity.
    LY334370 hydrochloride
  • HY-116790BS
    (±)-Penbutolol-d9
    (±)-Penbutolol-d9 is the deuterium labeled (±)-Penbutolol.
    (±)-Penbutolol-d<sub>9</sub>
  • HY-14546S1
    Aripiprazole (1,1,2,2,3,3,4,4-d8)
    Agonist
    Aripiprazole (1,1,2,2,3,3,4,4-d8) is the deuterium labeled Aripiprazole. Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
    Aripiprazole (1,1,2,2,3,3,4,4-d<sub>8</sub>)
  • HY-A0019S
    Paliperidone-d4
    Antagonist
    Paliperidone-d4 is the deuterium labeled Paliperidone. Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
    Paliperidone-d<sub>4</sub>
  • HY-17038S1
    Agomelatine-d4
    Antagonist
    Agomelatine-d4 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
    Agomelatine-d<sub>4</sub>
  • HY-B0500AS
    Alverine-d5 citrate
    98.52%
    Alverine-d5 (citrate) is the deuterium labeled Alverine citrate.
    Alverine-d<sub>5</sub> citrate
  • HY-17410S
    Iloperidone-d3
    Antagonist
    Iloperidone-d3 is the deuterium labeled Iloperidone. Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.
    Iloperidone-d<sub>3</sub>
  • HY-14264S
    Cyamemazine-d6
    Antagonist
    Cyamemazine-d6 is the deuterium labeled Cyamemazine. Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.
    Cyamemazine-d<sub>6</sub>
  • HY-B0383AS
    Almotriptan hydrochloride-d6
    Almotriptan-d6 hydrochloride is the deuterium labeled Almotriptan. Almotriptan is a 5-HT1B/1D-receptor agonist used to treat migraine.
    Almotriptan hydrochloride-d<sub>6</sub>
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