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

PDF 7.25 MB

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-117799
    LY-426965
    		Antagonist
    LY426965 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
  • HY-A0171
    Benzoctamine
    		Inhibitor
    Benzoctamine is an orally active and potent psychoactive agent which possesses tranquillizing properties. Benzoctamine increases the turnover rate of catecholamines. Benzoctamine enhances the [3H]noradrenaline uptake in the rat heart. Benzoctamine also accelerated the disappearance of intracisternally injected [3H]noradrenaline.
    Benzoctamine
  • HY-183577
    5-HT2A agonist 10
    		Agonist
    5-HT2A agonist 10 is a 5-HT2A receptor agonist with an EC50 of 9 nM. 5-HT2A agonist 10 is applicable to research related to central nervous system diseases.
    5-HT2A agonist 10
  • HY-138257
    (S)-Indeloxazine benzenesulfonate
    		Inhibitor
    (S)-AS1069562 is the S-enantiomer of AS1069562 (HY-138257A). AS1069562 is an orally active 5-HT and NE reuptake inhibitor, with IC50 values of 0.35 μM and 3.3 μM, respectively. AS1069562 possesses curative-like analgesic effect. AS1069562 might improve nerve function impairment via the amelioration of neurotrophic support.
    (S)-Indeloxazine benzenesulfonate
  • HY-14262S1
    Vilazodone-d8 hydrochloride
    		Agonist
    Vilazodone-d8 hydrochloride is deuterated labeled Vilazodone (HY-14262). Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
    Vilazodone-d<sub>8</sub> hydrochloride
  • HY-B1562
    Bopindolol
    Bopindolol ((±)-Bopindolol) is an orally active antagonist of β-adrenoceptors (ARs) with partial agonist activity. Bopindolol is non-selective for β1- and β2-ARs and has low affinity for β3-AR subtype. Bopindolol has intrinsic sympathomimetic as well as membrane stabilizing actions, inhibits renin secretion, and interacts with 5-HT receptors. Bopindolol is a proagent of Pindolol (HY-B0982). Bopindolol can be used for essential and renovascular hypertension research.
    Bopindolol
  • HY-117063
    LEK 8841 methanesulfonate
    LEK 8841 methanesulfonate is a gastrointestinal calming agent with strong selective 5-HT2 receptor antagonist activity. The antipsychotic potential of LEK 8841 has made it the focus of research into alternative medicines. LEK 8841 behaves as a pure competitive antagonist in response to 5-HT and norepinephrine, with pA2 values of 7.93 and 6.45, respectively. The selectivity of LEK 8841 is better than that of the comparative drug ketanserin, making it an important reference value in corresponding receptor research. Studies related to structural modifications have shown that LEK 8841 exhibits high affinity for 5-HT2 receptors and low alpha-adrenergic receptor activity.
    LEK 8841 methanesulfonate
  • HY-146076
    5-HT6/5-HT2A receptor ligand-1
    		Antagonist
    5-HT6/5-HT2A receptor ligand-1 (compound 33) is a dual 5-HT6/5-HT2A receptor antagonist, with a Ki of 2 nM and 11 nM, respectively. 5-HT6/5-HT2A receptor ligand-1 has the potential for neurological and psychiatric disorders research.
    5-HT6/5-HT2A receptor ligand-1
  • HY-121562
    SB 714786
    		Antagonist
    SB 714786 is a potent and selective 5-hydroxytryptamine 1D (5-HT1D) receptor antagonist. It was developed from the previously reported series of dual 5-HT1 selective 5-hydroxytryptamine reuptake inhibitors (5HT1-SSRIs). SB 714786 is the first reported highly potent and selective 5-HT1D receptor antagonist, providing an extremely useful pharmacological tool for further understanding the role of 5-HT1 receptor subtypes. It has no or very low intrinsic activity against all three receptors. SB 714786 has pKi values of 6.5, 6.7, 9.1 and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D and SerT receptors, respectively, showing high selectivity for 5-HT1D receptors. These properties make SB 714786 a potential tool compound for studying the function of 5-HT1D receptors and the treatment of related diseases.
    SB 714786
  • HY-15414S
    Vortioxetine-d8
    		Inhibitor
    Vortioxetine-d8 (Lu AA 21004-d8) is a deuterated version of Vortioxetine. Vortioxetine (Lu AA 21004) is an antagonist of 5-HT3A and 5-HT7 receptors (Ki: 3.7 nM, 19 nM) and an inhibitor of 5-hydroxytryptamine transporter (SERT) (Ki: 1.6 nM), as well as a 5-HT1A agonist and a partial 5-HT1B agonist (Ki: 15 nM, 33 nM).
    Vortioxetine-d<sub>8</sub>
  • HY-175657
    5-HT2A receptor agonist-12
    		Agonist
    5-HT2A receptor agonist-12 (compound 161-2) is a potent 5-HT2A agonist with an EC50 value of <100 nM for h5-HT2A.
    5-HT2A receptor agonist-12
  • HY-B0352S3
    Mirtazapine-d4 hydrochloride
    		Antagonist
    Mirtazapine-d4 hydrochloride is deuterated labeled Mirtazapine (HY-B0352). Mirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
    Mirtazapine-d<sub>4</sub> hydrochloride
  • HY-180379
    Pelanserin
    		Antagonist
    Pelanserin (Compound 1) is an orally active antihypertensive agent. Pelanserin is a potent 5-HT2 receptor antagonist. Pelanserin has the ability to block the activity of α-adrenergic receptor, with its ED50 being 0.03 μg/mL. Pelanserin has vasodilatory activity, with its ED100 being 5 μg. Pelanserin exhibits antihypertensive activity in hypertensive rats and renal hypertensive dog breeds. Pelanserin can be used for research on hypertension.
    Pelanserin
  • HY-127141
    Cizolirtine citrate
    		Agonist
    Cizolirtine citrate (E-4018) is an analgesic agent. Cizolirtine citrate has significant analgesic and anti-hyperalgesic action in neuropathic pain models.
    Cizolirtine citrate
  • HY-167893
    AGH-107
    		Agonist
    AGH-107 is a high selective and brain-penetrant agonist of 5-HT7 receptor, with a Ki of 6 nM and EC50 of 19 nM. AGH-107 exhibits high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.
    AGH-107
  • HY-114178
    CDK8-IN-2
    CDK8-IN-2 is an orally active CDK8 inhibitor of an IC50 values of 0.010 μM. CDK8-IN-2 shows a CDK19 IC50 value of 0.026 μM. CDK8-IN-2 inhibits phospho-STAT1, a pharmacodynamic biomarker of CDK8. CDK8-IN-2 inhibits WNT pathway activity. CDK8-IN-2 can be used for the research of colorectal carcinoma.
    CDK8-IN-2
  • HY-155215
    Tenilapine
    		Antagonist
    Tenilapine displays potent inverse agonist activity at rat and human 5-HT(2C) receptors.
    Tenilapine
  • HY-170908
    Pellotine
    		Antagonist
    Pellotine is an alkaloid that can be isolated from Lophophora. Pellotine is the inverse agonist for 5-HT7 receptor with an EC50 of 291 nM. Pellotine exhibits good affinity to 5-HT1DR and 5-HT6R with Ki of 117 nM and 170 nM. Pellotine reduces intracellular cAMP levels, thereby reducing neuronal excitability and neurotransmitter release.
    Pellotine
  • HY-174146
    5-HT1A agonist 1
    		Agonist
    5-HT1A agonist 1 (Compound Ex.37) is a highly selective 5-HT1a receptor agonist (EC50=0.18 nM). 5-HT1A agonist 1 mimicks serotonin binding to the receptor, promotes postsynaptic membrane hyperpolarization, inhibits neuronal hyperexcitability, and reduces the release of anxiety-related neurotransmitters. 5-HT1A agonist 1 is promising for research of neuropsychiatric diseases.
    5-HT1A agonist 1
  • 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>
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.