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-167648
    PD 158771
    		Agonist
    PD 158771 is an antipsychotic agent that functions as a partial agonist for D2 /D3 receptors (Ki = 42.0/13.7 nM) and as an agonist for 5-HT1A receptors (Ki = 2.6 nM). PD 158771 can be utilized in antipsychotic research.
    PD 158771
  • HY-A0157A
    Dimethothiazine mesylate
    		Antagonist
    Dimethothiazine mesylate is an orally active tricyclic anti-histamine, anti-5-HT agent with a high activity against decerebrate rigidity, a little sedative activity and little soporific action. Dimethothiazine mesylate can reduce or abolish the effects of both static and dynamic fusimotor activity on the muscle spindle in decerebrate cat. Dimethothiazine mesylate can be used to research hemicrania and spasticity.
    Dimethothiazine mesylate
  • HY-148718R
    4-Chloro Trazodone hydrochloride (Standard)
    		Control
    4-Chloro Trazodone (hydrochloride) (Standard) is the analytical standard of 4-Chloro Trazodone (hydrochloride). This product is intended for research and analytical applications. 4-Chloro Trazodone hydrochloride is an isomer of Trazodone hydrochloride (HY-B0478). Trazodone hydrochloride is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
    4-Chloro Trazodone hydrochloride (Standard)
  • HY-135241
    25I-NBF hydrochloride
    		Agonist
    25I-NBF hydrochloride is a highly potent partial agonist for the 5-HT2A receptors receptor with a Ki value of 0.26 nM and an EC50 value of 1.6 nM.
    25I-NBF hydrochloride
  • HY-B1213AR
    Trimipramine (Standard)
    		Antagonist
    Trimipramine (Standard) is the analytical standard of Trimipramine. This product is intended for research and analytical applications. Trimipramine is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine has vascular activity and anxiolytic efficacy.
    Trimipramine (Standard)
  • HY-10121S2
    Asenapine-13C,d3
    		Antagonist
    Asenapine-13C,d3 is 13C and deuterated labeled Asenapine (HY-10121). Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
    Asenapine-<sup>13</sup>C,d<sub>3</sub>
  • HY-123272
    E6801
    		Agonist
    E6801 is a 5-HT6 receptor agonist that improves recognition memory by jointly modulating cholinergic and glutamatergic neurotransmission. E6801 can be used in studies of dementia, depression, obesity, epilepsy, etc.
    E6801
  • HY-165624B
    (R)-LY-41
    		Agonist
    (R)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (R)-LY-41 is a potent and selective 5-HT1A receptor agonist. (R)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (R)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (R)-LY-41 can induce the 5-HT behavioral syndrome but is weaker than (S)-LY-41 (HY-165624A). (R)-LY-41 can be used for the research of neurological disease, such as depression and anxiety.
    (R)-LY-41
  • HY-156533
    5-HT2 agonist-1
    		Agonist
    5-HT2 agonist-1 (Compound 24) is a 5-HT2A & 5-HT2B & 5-HT2C agonist, with IC50s of 10 nM, 8.3, and 1.6 nM respectively. 5-HT2 agonist-1 free base can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.
    5-HT2 agonist-1
  • HY-182695
    AS2030680
    		Antagonist
    AS2030680 is a blood-brain barrier-permeable, orally active 5-HT5A receptor antagonist. AS2030680 regulates 5-HT5A-related downstream signaling pathways, reduces the frequency of tumorsphere-initiating cells in breast cancer cells, and exerts procognitive activity in animal models. AS2030680 can be used to study cognitive impairments associated with dementia and schizophrenia, as well as breast cancer.
    AS2030680
  • HY-B0019
    Azasetron
    Azasetron ((Rac)-SENS-401 free base) is an antiemetic drug with 5-HT3 receptor antagonist activity. Azasetron is often used as a preventive measure for postoperative nausea and vomiting or chemotherapy-induced nausea and vomiting. Azasetron does not impair neutrophil chemotaxis or phagocytosis and does not scavenge O(-)(2) or H(2)O(2) generated by cell-free systems.
    Azasetron
  • HY-103107B
    LY334370 fumarate
    		Agonist
    LY334370 fumarate is the fumarate of LY334370 (HY-103107). LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.
    LY334370 fumarate
  • HY-175822
    5-HT2A inverse agonist-1
    		Inhibitor
    5-HT2A inverse agonist-1 is a 5-HT2A receptor inverse agonist with a IC50 of 5.5 nM. 5-HT2A inverse agonist-1 shows minimal hERG inhibition. 5-HT2A inverse agonist-1 can be used for the research of neurological disease, such as Parkinson’s disease.
    5-HT2A inverse agonist-1
  • HY-117507
    U92016A hydrochloride
    		Agonist 99%
    U92016A hydrochloride is a potent, metabolically stable, orally acitive 5-HT1A receptor agonist with an exceptionally high degree of intrinsic activity. U92016A hydrochloride binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells (Ki=0.2 nM).
    U92016A hydrochloride
  • HY-117799A
    LY-426965 hydrochloride
    		Antagonist
    LY-426965 hydrochloride is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders.
    LY-426965 hydrochloride
  • HY-15401
    WAY 163909
    		Agonist
    WAY 163909 is an orally active, blood-brain barrier permeable 5-HT2C receptor-selective agonist. WAY 163909 exhibits an EC50 of 8 nM and a Ki of 10.5 nM for h5-HT2C. Instead of triggering apoptosis, WAY 163909 induces anorectic, antipsychotic-like, antidepressant-like, anti-aggressive and anti-compulsive effects. WAY 163909 alleviates ketamine-induced hypothermia, but impairs sexual function at high doses. With rapid antidepressant-like properties, WAY 163909 can be used in research related to obesity, schizophrenia, depression, obsessive-compulsive disorder, and anesthesia-induced hypothermia.
    WAY 163909
  • HY-14153S
    Tegaserod-d11
    		Agonist
    Tegaserod-d11 is deuterated labeled Tegaserod (HY-14153). Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
    Tegaserod-d<sub>11</sub>
  • HY-100171
    PRX933 hydrochloride
    		Agonist
    PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1.
    PRX933 hydrochloride
  • HY-172679
    PUC-55
    		Inhibitor
    PUC-55 is a 5-HT6R antagonist with a Ki of 37.5 nM that induces neuronal autophagy by inhibiting the mTOR pathway. It holds potential for research in the field of neurological disorders.
    PUC-55
  • HY-155116
    5-HT6 agonist 1
    		Agonist
    5-HT6 agonist 1 (Compound 19) is a 5-HT6 agonist (Ki: 5 nM). 5-HT6 agonist 1 has antidepressant-like properties, and improves cognitive deficits. 5-HT6 agonist 1 also inhibits platelet aggregation. 5-HT6 agonist 1 has high metabolic stability.
    5-HT6 agonist 1
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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