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-119103B
    PF-03246799 monohydrochloride
    		Agonist
    PF-03246799 monohydrochloride is a potent and selective 5-HT2C receptor agonist with an EC50 of 190 nM and a Ki of 160 nM. PF-03246799 monohydrochloride shows selectivity for 5-HT2C over 5-HT2A and 5-HT2B receptors. PF-03246799 monohydrochloride has the potential for stress urinary incontinence (SUI) research.
    PF-03246799 monohydrochloride
  • HY-116982
    BMY 7378 free base
    		Agonist
    BMY 7378 (free base) is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 (free base) binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 (free base) is a 5-HT1A receptor partial agonist.
    BMY 7378 free base
  • HY-103105
    LP 12 hydrochloride
    		Agonist
    LP 12 hydrochloride (compound 21) is a potent and selective 5-HT7 receptor agonist with a Ki of 0.13 nM. LP 12 hydrochloride displays selectivity for 5-HT7 over D2, 5-HT1A and 5-HT2A receptors (Ki values are 224 nM, 60.9 nM and >1000 nM, respectively).
    LP 12 hydrochloride
  • HY-138906
    25C-NBF hydrochloride
    		Agonist
    25C-NBF hydrochloride is an agonist of 5-HT receptors that activates 5-HT2A and 5-HT2C similarly (EC50s = ~0.3 μM for each).
    25C-NBF hydrochloride
  • HY-108139
    F-14258
    		Agonist
    F-14258 is a 5-HT1B/1D receptor agonist. F-14258 can achieve receptor specific analgesia through local administration. F-14258 can be used for research on ear pain.
    F-14258
  • HY-182389
    NLX-219
    		Agonist
    NLX-219 is a selective agonist of the 5-HT1A with a pKi of 10.21. NLX-219 activates ERK1/2 phosphorylation, inhibits adenylyl cyclase activity, promotes β-arrestin recruitment. NLX-219 can be used for the research of neurological disease.
    NLX-219
  • HY-W746031
    WAY-181187 hydrochloride
    		Agonist
    WAY-181187 (SAX-187) hydrochloride is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 hydrochloride mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
    WAY-181187 hydrochloride
  • HY-14547
    Bifeprunox
    		Agonist
    Bifeprunox is a potent dopamine D2-like and 5-HT1A receptor partial agonist with pKis of 7.19 and 8.83 for cortex 5-HT1A and striatum D2, and a pEC50 of 6.37 for hippocampus 5-HT1A, respectively. Bifeprunox is an antipsychotic for the research of schizophrenia.
    Bifeprunox
  • HY-19863A
    F-15599 tosylate
    		Agonist
    F-15599 tosylate is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
    F-15599 tosylate
  • HY-169001
    5-HT2A/5-HT2C inverse agonist 1
    		Agonist
    5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2C receptor inverse agonist with a hERG inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis.
    5-HT2A/5-HT2C inverse agonist 1
  • HY-103110A
    ST1936 oxalate
    		Agonist
    ST1936 oxalate is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 oxalate also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
    ST1936 oxalate
  • HY-169825
    (S)-PF-04995274
    		Agonist
    (S)-PF-04995274 is a partial agonist of the 5-hydroxytryptamine receptor 4 (5-HT4R) and is an isomer of PF-04995274 (HY-18137).
    (S)-PF-04995274
  • HY-110024A
    S-14506
    		Agonist
    S-14506 hydrochloride is a potent 5-HT1A agonist. S-14506 hydrochloride displays dopamine antagonist properties by blocking dopamine D2 receptors. S-14506 hydrochloride inhibits the in vivo binding of [3H]raclopride in striatum and olfactory bulbs. S-14506 hydrochloride has the potential for the research of anxiolytic agent.
    S-14506
  • HY-120688
    L-772405
    		Agonist
    L-772405 is a selective 5-HT1D receptor agonist with the Ki values of 318, 29 and ＞ 1000 nM aganist guinea pig 5-HT1B receptor, guinea pig 5-HT1D receptor and rat 5-HT rransporter, respectively. L-772405 decreases the potassium-induced outflow of 5-HT with an IC50 value of 240 nM.
    L-772405
  • HY-176721
    5-HT2A receptor agonist-10
    		Agonist
    5-HT2A receptor agonist-10 (Compound (R)-I-121.HCl) is a 5-HT2A receptor agonist, with an IC50 of 2192.39 nM for h5-HT2A and h5-HT1A, respectively. 5-HT2A receptor agonist-10 can be used for the research of psychosis, mental illnesses and CNS disorders.
    5-HT2A receptor agonist-10
  • HY-162585
    5-HT1AR agonist 1
    		Agonist
    5-HT1AR agonist 1 (Compound A3) emerges as a relatively balanced multi-target activity profile, including 5-HT1AR agonist with an EC50 value of 34 nM, SERT reuptake ihibitor (IC50 =12 nM), NET reuptake inhibitor (IC50 =78 nM) and DAT reuptake inhibitor (IC50 =135 nM). 5-HT1AR agonist 1 performs significant antidepressant effects and exhibits excellent bioavailability and low clearance in mice, which is promising for research in the field of antidepressant drugs.
    5-HT1AR agonist 1
  • HY-176717
    5-HT1AR agonist 3
    		Agonist
    5-HT1AR agonist 3 (Compound 77) is a 5-HT1A agonist. 5-HT1AR agonist 3 has 5-HT1A receptor agonist activity (EC50: 1.3 nM). 5-HT1AR agonist 3 mainly exerts its effects by activating 5-HT1A receptors and can be used in the study of neuropsychiatric diseases such as anxiety, depression and sleep disorders.
    5-HT1AR agonist 3
  • HY-13221A
    BRL 54443 maleate
    		Agonist
    BRL 54443 (MALEATE) is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.
    BRL 54443 maleate
  • HY-B0031S5
    Quetiapine-d4-1 fumarate
    		Agonist
    Quetiapine-d4-1 fumarate is deuterated labeled Quetiapine (hemifumarate) (HY-B0031). Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
    Quetiapine-d<sub>4</sub>-1 fumarate
  • HY-130351
    25H-NBOMe hydrochloride
    		Agonist
    25H-NBOMe hydrochloride is an agonist for the rat and human serotonin 5-HT2A receptors with Ki values of 1.19 and 2.83 nM, respectively.
    25H-NBOMe hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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