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-106904
    Nexopamil
    		Antagonist
    Nexopamil is a calcium antagonist of Ca2+ channel, 5HT2, 5HT1A, 5HT1C and dopamine D2 receptors. Nexopamil exhibits vasodilatory, cardioprotective, and platelet aggregation inhibiting effects. Nexopamil can be used for researches of stable or unstable angina and possibly of peripheral arterial occlusive disease.
    Nexopamil
  • HY-173044
    5-HT1AR/5-HT6R ligand-1
    		Ligand
    5-HT1AR/5-HT6R ligand-1 (Compound PP13) is the ligand for 5-HT receptor that exhibits good affinity to 5-HT1AR, 5-HT6R and 5-HT7R (Ki of 19, 69 and 198 nM, respectively), thereby inhibiting the cAMP production in HEK293 cell with EC50 of 1535, 488 and 53 nM, respectively. 5-HT1AR/5-HT6R ligand-1 exhibits anti-proliferative activity against a variety of cancer cells (IC50 for 1321N1, U87MG, MCF7, and AsPC-1 is 9.6, 13.6, 19.3 and 14.6 μM, respectively). 5-HT1AR/5-HT6R ligand-1 also exhibits antagonist activity for dopamine receptor D2R with Ki of 1903 nM.
    5-HT1AR/5-HT6R ligand-1
  • HY-B1622S
    Cyproheptadine-d3
    Cyproheptadine-d3 is deuterium labeled Cyproheptadine.
    Cyproheptadine-d<sub>3</sub>
  • HY-106418A
    SGB-1534 hydrochloride
    		Antagonist
    SGB-1534 hydrochloride is an orally active, selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. SGB-1534 hydrochloride can inhibit vasoconstriction and lower blood pressure. SGB-1534 hydrochloride can be used for the research of cardiovascular disease, such as hypertension.
    SGB-1534 hydrochloride
  • HY-136678
    SB 258741
    		Antagonist
    SB 258741 is an efficient and highly selective 5-HT7 receptor (pKi = 8.
    SB 258741
  • HY-120627
    BMS-442606
    		Agonist
    BMS-442606, the S-enantiomer of 6-hydroxybuspirone (6OHB), is an orally active 5-HT1A partial agonist. BMS-442606 can be used for generalized anxiety disorder (GAD) research.
    BMS-442606
  • HY-146077
    5-HT6/5-HT2A receptor ligand-2
    		Antagonist
    5-HT6/5-HT2A receptor ligand-2 (compound 42) is a brain-penetrant dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 25 nM and 32 nM, respectively. 5-HT6/5-HT2A receptor ligand-2 shows pro-cognitive properties.
    5-HT6/5-HT2A receptor ligand-2
  • HY-N0775R
    Isocorynoxeine (Standard)
    		Inhibitor
    Isocorynoxeine (Standard) is the analytical standard of Isocorynoxeine. This product is intended for research and analytical applications. Isocorynoxeine, an isorhynchophylline-related alkaloid, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM.
    Isocorynoxeine (Standard)
  • HY-100171A
    PRX933
    		Agonist
    PRX933 (BVT-933) is a 5-HT2C agonist that can be used in the study of obesity and glaucoma.
    PRX933
  • HY-106605S
    Flumezapine-d8 hydrochloride
    		Antagonist
    Flumezapine-d8 (LY 120363-d8) hydrochloride is deuterated labeled Flumezapine hydrochloride. Flumezapine hydrochloride is a potent and balanced antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine receptor (5-HT receptor). Flumezapine hydrochloride does not alter the increase in serum cortisol caused by κ-opioid receptor agonists. Flumezapine hydrochloride inhibits the conditioned avoidance response in rats and has a low risk of extrapyramidal side effects. Flumezapine hydrochloride can be used in antipsychotic research.
    Flumezapine-d<sub>8</sub> hydrochloride
  • HY-169394
    5-HT1AR agonist 2
    		Agonist
    5-HT1AR agonist 2 (Compound 4f) is a 5-HT1A receptor agonist (Ki: 10.0 nM). 5-HT1AR agonist 2 also binds to the SERT, D2 receptor and 5-HT6 receptor (Ki: SERT, 2.8 nM; D2, 23 nM; 5-HT6, 192 nM). 5-HT1AR agonist 2 is stabilized in microsomes and induces hypothermia in mice.
    5-HT1AR agonist 2
  • HY-148032
    5-Benzyloxytryptamine
    		Agonist
    5-Benzyloxytryptamine (5-BT) is a selective partial agonist for 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors with an IC50 value of 40 nM for bovine caudate 5-HT1D and reduced affinity for other receptors (5-HT2 IC50>470 nM). 5-Benzyloxytryptamine inhibits adenylate cyclase to decrease neurotransmitter release and downregulate cAMP signaling. 5-Benzyloxytryptamine is promising for research of neurotransmitter imbalance-related disorders like migraine.
    5-Benzyloxytryptamine
  • HY-101225
    8 Hydroxy PIPAT oxalate
    		Agonist
    8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that promotes the release of histamine from enteric mast cells. 8 Hydroxy PIPAT oxalate activates serotonergic signaling pathways, leading to the degranulation of mast cells in both guinea pig and human intestinal preparations. 8 Hydroxy PIPAT oxalate enhances the spontaneous release of histamine, which may contribute to the regulation of gastrointestinal functions. 8 Hydroxy PIPAT oxalate has potential implications for understanding and treating functional gastrointestinal disorders such as irritable bowel syndrome.
    8 Hydroxy PIPAT oxalate
  • HY-15394A
    (Rac)-Rotigotine
    		Agonist
    (Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    (Rac)-Rotigotine
  • HY-136860
    (R)-Venlafaxine
    		Inhibitor
    (R)-Venlafaxine is the R-enantiomer of venlafaxine (HY-B0196), an orally active and potent dual inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake. (R)-Venlafaxine can be utilized in antidepressant research.
    (R)-Venlafaxine
  • HY-171052
    5-HT6R antagonist 5
    		Antagonist
    5-HT6R antagonist 5 (compound 1.2.12(4)) is a potent competitive 5-HT6R antagonist with an IC50 of 4.19 nM. 5-HT6R antagonist 5 can be used for research in various central nervous system (CNS) diseases, cognitive and neurodegenerative diseases.
    5-HT6R antagonist 5
  • HY-121053
    Adatanserin
    		Modulator
    Adatanserin (WY-50324) is a high affinity, selective and partial agonist for the 5-HT1A receptor with a Ki of 1 nM. Adatanserin is a moderate affinity 5-HT2 receptor antagonist with a Ki of 73 nM. Adatanserin shows significant anxiolytic and antidepressant activity in an animal conflict model.
    Adatanserin
  • HY-14782A
    Adoprazine hydrochloride
    		Agonist
    Adoprazine (SLV313) hydrochloride is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine hydrochloride is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine has the characteristics of atypical antipsychotics.
    Adoprazine hydrochloride
  • HY-A0039
    Eletriptan
    		Agonist
    Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine.
    Eletriptan
  • HY-106578
    Quinupramine
    Quinupramine is an orally active antidepressant. Quinupramine can penetrate into the CNS and affect some of the processes of neurotransmission. The antidepressant activity of quinupramine is associated with the central serotonin system, but not with the β-adrenergic system[1][2].
    Quinupramine
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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