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-169467
    5-Chloro-α-methyltryptamine
    		Agonist
    5-Chloro-α-methyltryptamine (Compound 7b) is a potent and selective dual DA/5-HT releaser and 5-HT2a agonist. 5-Chloro-α-methyltryptamine releases DA and 5-HT with the EC50 values of 54.3 nM and 16.2 nM, respectively. 5-Chloro-α-methyltryptamine can be used in the study of neurotransmitter.
    5-Chloro-α-methyltryptamine
  • HY-14153AS
    Tegaserod-13C,d3 maleate
    		Modulator
    Tegaserod-13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract.
    Tegaserod-<sup>13</sup>C,d<sub>3</sub> maleate
  • HY-103113
    MS 245 oxalate
    		Antagonist
    MS 245 oxalate is a potent antagonist of 5-HT6 receptor with a Ki of 2 nM.
    MS 245 oxalate
  • HY-180465
    5-HT2C agonist-12
    		Agonist
    5-HT2C agonist-12 (example.2) is a selective and orally active 5-HT2C receptor agonist. 5-HT2C agonist-12 can inhibit the accumulation of IP3 with an IC50 of 4.5 nM. 5-HT2C agonist-12 can induce a feeling of fullness, shorten the time of eating, and reduce calorie intake. 5-HT2C agonist-12 can be used for the research of obesity.
    5-HT2C agonist-12
  • HY-108973A
    Ifoxetine
    		Inhibitor
    Ifoxetine (CGP 15210G) is an inhibitor of 5-HT reuptake. Ifoxetine specifically and selectively blocks the 5-HT reuptake in the brain without affecting the 5-HT uptake processes in the periphery (blood platelets). Ifoxetine inhibits the uptake of radiolabelled 5-HT into rat brain synaptosomes in vitro or ex vivo. Ifoxetine has antidepressant properties.
    Ifoxetine
  • HY-16688B
    RU 24969 hemisuccinate
    		Agonist
    RU 24969 hemisuccinate is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 hemisuccinate could decrease fluid consumption and increase forward locomotion.
    RU 24969 hemisuccinate
  • HY-19252
    GR-4991W93
    		Agonist
    GR-4991W93 is an orally active partial agonist against 5HT1B/1D receptor, with pIC50 values of 6.95 and 7.80 against 5HT1B and 5HT1D, respectively. GR-4991W93 demonstrates potent inhibition of electrically evoked plasma extravasation in the guinea pig. GR-4991W93 can be used for migraine research.
    GR-4991W93
  • HY-103403
    (-)-OSU6162 hydrochloride
    		Agonist
    (-)-OSU6162 (PNU96391) hydrochloride is a dopamine stabilizer. (-)-OSU6162 hydrochloride acts as partial agonist at 5-HT2A and is a dopamine D2 antagonist. (-)-OSU6162 hydrochloride can be used for the research of aggression and irritability.
    (-)-OSU6162 hydrochloride
  • HY-156532A
    5-HT2C agonist-3 free base
    		Agonist
    5-HT2C agonist-3 ((+)-19) free base is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 free base has antipsychotic drug-like activity. 5-HT2C agonist-3 free base blocks Amphetamine-induced hyperactivity.
    5-HT2C agonist-3 free base
  • HY-101100A
    Anpirtoline
    		Agonist
    Anpirtoline (D-16949) is a centrally acting 5-HT1B receptor agonist, with Kis of 28 nM (5-HT1B), 150 nM (5-HT1A) and 1.49 μM (5-HT2). Anpirtoline has serotonergic, antinociceptive, antidepressant-like effects.
    Anpirtoline
  • HY-103116
    DV-7028 hydrochloride
    		Antagonist
    DV-7028 is a selective 5-hydroxytryptamine2 (5-HT2) receptor antagonist.
    DV-7028 hydrochloride
  • HY-18138
    PF-03382792
    		Agonist 99.58%
    PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex.
    PF-03382792
  • HY-156807
    LY 367265
    		Antagonist
    LY 367265 is a 5-hydroxytryptamine transporter (SERT) inhibitor (IC₅₀ = 3.1 nM) and a 5-HT₂A receptor antagonist (Kᵢ = 0.81 nM). LY 367265 has the inhibitory activity on the norepinephrine transporter (NET) of extremely weak (IC₅₀ > 1000 nM); it has low affinity for subtypes such as 5-HT₁B (Kᵢ = 490 nM) and 5-HT₁D (Kᵢ = 81 nM), showing high selectivity. LY 367265 concentration-dependently enhances of [³H]5-HT efflux (EC₅₀ = 250 nM). LY 367265 antagonizes the contraction response of Sumatriptan (HY-B0121B), indicating its functional antagonistic activity on 5-HT₁D-like receptors. LY 367265 can be used for the study of diseases such as anxiety disorders and post-traumatic stress disorder.
    LY 367265
  • HY-106928
    U 93385
    		Agonist
    U93385 is a 5-HT₁A receptor agonist. U93385 exhibits no significant α₂ adrenergic, D₂ dopamine, or other receptor activities. U93385 has a heart rate regulating effect, stimulating the vagus nerve to induce bradycardia. U93385 can be used to study the 5-HT₁A receptor-mediated vagal nerve tolerance mechanism.
    U 93385
  • HY-103092
    CP-135807
    		Agonist
    CP-135807 is an orally active and selective 5-HT1D agonist (IC50=3.1 nM), bovine). CP-135807 mediates central psychoactivity and can be used in antidepressant research.
    CP-135807
  • HY-W743888
    AL-LAD
    		Activator
    AL-LAD (6-Allyl-6-nor-LSD) is an activator for 5-HT2A receptor with Ki of 3.4-8.1 nM. AL-LAD exhibits affinity for dopamine receptor D1 and dopamine receptor D2 with absolute affinitiesK0.5 of 189 nM and 12.3 nM. AL-LAD acts as psychoactive substance in mouse model.
    AL-LAD
  • HY-B0032S
    Lurasidone-d8 hydrochloride
    		Antagonist
    Lurasidone-d8 (hydrochloride) is the deuterium labeled Lurasidone, which is an inhibitor of Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C.
    Lurasidone-d<sub>8</sub> hydrochloride
  • HY-19686A
    Ipsapirone hydrochloride
    		Modulator
    Ipsapirone hydrochloride (TVX Q 7821) is an anxiolytic compound and a 5-HT1A receptor partial agonist. Ipsapirone hydrochloride (TVX Q 7821) also exhibits 5-HT1A receptor antagonistic effect, and only at high doses it can also produce an inhibitory effect on 5-HT2 and the α1-adrenergic function.
    Ipsapirone hydrochloride
  • HY-101365
    RS-102221
    		Antagonist
    RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats.
    RS-102221
  • HY-172258
    5-HT2B antagonist-2
    		Inhibitor
    5-HT2B antagonist-2 (Compound 19c) is a 5HT2B receptor antagonist with an IC50 of 1.09 nM. 5-HT2B antagonist-2 can downregulate the expression of fibrosis-related genes α-SMA, Timp1, Col1a1, and Col3a1, and significantly reduce the deposition of fibrosis, thereby reducing the fibrotic area and inhibiting the fibrotic process in CCl4-induced liver fibrosis mouse models. 5-HT2B antagonist-2 can be used in the study of immune inflammatory-related diseases, particularly in the research of pulmonary fibrosis diseases.
    5-HT2B antagonist-2
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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