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-14558S
    Tandospirone-d8
    		Agonist
    Tandospirone-d8 (SM-3997-d8) is deuterium labeled Tandospirone. Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms.
    Tandospirone-d<sub>8</sub>
  • HY-124947
    PF-4522654
    		Agonist
    PF-4522654 is a potent, selective and brain-permeable 5-HT2C receptor agonist with an EC50 of 16 nM and a Ki of 8 nM. PF-4522654 shows no measurable functional agonism at no 5-HT2A and 5-HT2B receptors. PF-4522654 can be used for the study of stress urinary incontinence (SUI).
    PF-4522654
  • HY-181351
    PSN09
    		Agonist
    PSN09 is a blood-brain barrier-permeable agonist of PSAM4-GlyR and PSAM4-5-HT3 receptors with high affinity. 18F-labeled PSN09 serves as a radiotracer for PET imaging in non-human primates.
    PSN09
  • HY-119103
    PF-03246799
    		Agonist
    PF-03246799 is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 has the potential for stress urinary incontinence (SUI) research.
    PF-03246799
  • HY-103109
    Melperone hydrochloride
    		Antagonist
    Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values ​​of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly.
    Melperone hydrochloride
  • HY-W681014
    5-Fluoro-α-methyltryptamine hydrochloride
    		Activator
    5-Fluoro-α-methyltryptamine hydrochloride may cause an increase in intracellular levels of 5-HT followed by an increase in 5-HT release. 5-Fluoro-α-methyltryptamine hydrochloride exhibits EC50 values of 37 nM, 14 nM, 78 nM and 8.47 nM for DA, 5HT, NE and 5-HT2A, respectively.
    5-Fluoro-α-methyltryptamine hydrochloride
  • HY-105034A
    Tiospirone hydrochloride
    		Antagonist
    Tiospirone (MJ 13859-1) hydrochloride is an orally active antipsychotic agent that reduces or eliminates tardive dyskinesia (TD) in Cebus apella monkeys with persistent TD.
    Tiospirone hydrochloride
  • HY-112390C
    Syk Inhibitor II hydrochloride
    		Inhibitor
    Syk Inhibitor II hydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II hydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II hydrochloride shows less potent against other kinases and has anti-allergic effect.
    Syk Inhibitor II hydrochloride
  • HY-129850
    4-Chloromethamphetamine hydrochloride
    		Inhibitor
    4-Chloromethamphetamine hydrochloride is a new psychoactive substance belonging to the amphetamine class.
    4-Chloromethamphetamine hydrochloride
  • HY-101753A
    Cianopramine hydrochloride
    		Inhibitor
    Cianopramine hydrochloride (Cyanimipramine hydrochloride; Ro 11-2465 hydrochloride) is the hydrochloride form of Cianopramine (HY-101753). Cianopramine hydrochloride is an antidepressant, which selectively inhibits the serotonin uptake into synaptosomes.
    Cianopramine hydrochloride
  • HY-120810
    MCI-225 hydrate hydrochloride
    		Antagonist
    MCI-225 (DDP-225) hydrate hydrochloride is a selective and orally active noradrenaline (NA) reuptake inhibitor with 5-HT3 receptor antagonism. MCI-225 hydrate hydrochloride has antidepressant-like and anxiolytic-like properties. MCI-225 hydrate hydrochloride can be used for the study of anxiety disorder.
    MCI-225 hydrate hydrochloride
  • HY-W284026
    PIM-35
    		Inhibitor
    PIM-35 is a derivative of Indole (HY-W001132). PIM-35 significantly inhibits serotonin (5HT) and dopamine (DA) uptake with a weak inhibitory effect on noradrenaline (NA) uptake.PIM-35 has antidepressant activity and can be used for depression research.
    PIM-35
  • HY-181613
    5-HT2A&5-HT2C agonist-3
    		Agonist
    5-HT2A&5-HT2C agonist-3 is an orally active and blood-brain barrier penetrant 5-HT2A and 5-HT2C agonist, with pEC50 values of 7.79 and 7.10, respectively. 5-HT2A&5-HT2C agonist-3 elevates intracellular calcium levels in cells overexpressing 5-HT2A or 5-HT2C receptors, and shows no activity against 5-HT2B receptors. 5-HT2A&5-HT2C agonist-3 can be used in the research of neuropsychiatric disorders.
    5-HT2A&5-HT2C agonist-3
  • HY-186170B
    (R,S)-MDMA
    		Agonist
    (R,S)-MDMA acts as a partial agonist of 5-HT2A, 5-HT2B and 5-HT2C receptors. (R,S)-MDMA belongs to psychoactive substances. (R,S)-MDMA exhibits antidepressant activity. (R,S)-MDMA can be used for research on mental disorders such as post-traumatic stress disorder and depression.
    (R,S)-MDMA
  • HY-106507
    Batoprazine
    		Agonist
    Batoprazine (8-(1-piperazinyl)-2H-1-benzopyran-2-one)) is a 5-HT1A,1B receptor agonist. Batoprazine can replace the behavioral stimulus of eltoprazine in the two-lever operant discrimination test between eltoprazine and deionized water in rats (ED50: 0.20 mg/kg).
    Batoprazine
  • HY-133732
    Alaproclate hydrochloride
    		Inhibitor
    Alaproclate (GEA 654) hydrochloride is a selective and orally active serotonin re-uptake inhibitor (SSRI). Alaproclate hydrochloride also acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow.
    Alaproclate hydrochloride
  • HY-172982
    CTW0419
    		Modulator
    CTW0419 is a potent 5-HT Receptor positive allosteric modulators (PAMs). CTW0419 is promising for research of neuropsychiatric disorders.
    CTW0419
  • HY-103123
    SB 258719 hydrochloride
    		Antagonist
    SB 258719 hydrochloride is a selective 5-HT7 receptor antagonist displayed high affnity (pKi=7.5) for the receptor. SB-258719 hydrochloride can be used for the research of cancer and neurological diseases.
    SB 258719 hydrochloride
  • HY-44132
    Dehydro Palonosetron
    		Antagonist
    Dehydro Palonosetron (RS 42358-197) is a potent, seslective and orally active 5-HT3 receptor antagonist. Dehydro Palonosetron has no effect on the activities of 5-HT1 receptors, 5-HT2 receptors or 5-HT4 receptors.
    Dehydro Palonosetron
  • HY-183805
    5-HT6R/FAAH modulator 2
    		Antagonist
    5-HT6R/FAAH modulator 2 is a dual 5-HT6R antagonist and FAAH inhibitor with human 5-HT6R pKi 7.24, human FAAH pIC50 5.47, and blood-brain barrier penetration.5-HT6R/FAAH modulator 2 modulates serotonergic signaling, blocks 5-HT6R function, inhibits endocannabinoid degradation via FAAH catalytic activity suppression.5-HT6R/FAAH modulator 2 exhibits neuroprotective effects against mitochondrial dysfunction, amyloid-β, and glutamate-induced toxicity, reverses memory deficits.5-HT6R/FAAH modulator 2 shows reduced cytotoxicity relative to oxygen-containing lead compounds.5-HT6R/FAAH modulator 2 can be used for the research of Alzheimer's disease.
    5-HT6R/FAAH modulator 2
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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