2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

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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-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-115525
    NBUMP
    		Ligand
    NBUMP is a 5-HT1A receptor ligand with a 5-HT1A receptor Ki of 0.1 nM, α1-adrenergic receptor Ki of 46 nM, and a 5-HT1A receptor-to-α1-adrenergic receptor selectivity ratio of 460.NBUMP binds to the 5-HT1A receptor with high affinity.NBUMP binds to the α1-adrenergic receptor with lower affinity.
    NBUMP
  • 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-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-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 98.8%
    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-B0740S
    Cyclobenzaprine-d3 hydrochloride
    		Antagonist
    Cyclobenzaprine-d3 (hydrochloride) is the deuterium labeled Cyclobenzaprine hydrochloride. Cyclobenzaprine hydrochloride (MK130 hydrochloride) is a skeletal muscle relaxant and a central nervous system (CNS) depressant.
    Cyclobenzaprine-d<sub>3</sub> hydrochloride
  • 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-18610S
    Diclofensine-d3 (hydrochloride)
    		Inhibitor
    Diclofensine-d3 (Ro-8-4650-d3) hydrochloride is the deuterium labeled Diclofensine hydrochloride. Diclofensine hydrochloride is an orally active neuronal monoamine uptake inhibitor. Diclofensine hydrochloride blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine hydrochloride potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine hydrochloride produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine hydrochloride can be used in the research of moderate to severe depression.
    Diclofensine-d<sub>3</sub> (hydrochloride)
  • HY-B0121BS1
    Sumatriptan-d6
    Sumatriptan-d6 is the deuterium labeled Sumatriptan. Sumatriptan is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan can be used for migraine headache research.
    Sumatriptan-d<sub>6</sub>
  • HY-B0189S1
    Mosapride-d5
    		Agonist
    Mosapride-d5 is the deuterium labeled Mosapride. Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
    Mosapride-d<sub>5</sub>
  • HY-123129
    RS 2232
    RS 2232 is an orally active, competitive 5-HT deamination inhibitor with a Ki of 0.054 μM. RS-2232 exhibits reversible and specific inhibition of type A monoamine oxidase. RS 2232 can be used in brain research.
    RS 2232
  • HY-123207
    BP 554
    		Agonist
    BP 554 is a selective 5-HT1A receptor agonist and Piperazine derivative. BP 554 leads to hypothermia.
    BP 554
  • HY-B0750BR
    Dolasetron Mesylate hydrate (Standard)
    		Antagonist
    Dolasetron Mesylate hydrate (MDL-73147EF hydrate) (Standard) is the analytical standard of Dolasetron Mesylate hydrate (HY-B0750B). This product is intended for research and analytical applications. Dolasetron Mesylate hydrate is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
    Dolasetron Mesylate hydrate (Standard)
  • HY-181977
    RPI-GLYT2-82
    		Inhibitor
    RPI-GLYT2-82 is a reversible, blood-brain barrier-permeable allosteric inhibitor of GlyT2 with an IC50 value of 554 nM. RPI-GLYT2-82 also exhibits inhibitory activity against 5-HT2AR and SERT, with IC50 values of 1.9 μM and 4.7 μM, respectively. RPI-GLYT2-82 inhibits pain signals and alleviates allodynia, shows no target-related side effects at the maximum analgesic dose, and has no addictive potential. RPI-GLYT2-82 can be used for the research of neuropathic pain.
    RPI-GLYT2-82
  • HY-167238
    RS-30199
    		Modulator
    RS-30199 is an anxiogenic agent. RS-30199 interacts with the 5-HT1A receptor. RS-30199 prolongs intromission latency. RS-30199 fully inhibits the facilitation of sexual behaviour caused by Delequamine (HY-106874).
    RS-30199
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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