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-106805
    ICI 169369
    		Antagonist
    ICI 169369 is an orally active, specific serotonin and 5-HT2/5-HT1C receptor competitive antagonist. ICI 169369 exhibits Ki values of 1.79 x 10−8 and 1.58 x 10−6 M for 5-HT2 and 5-HT1, respectively.
    ICI 169369
  • HY-B0352BS
    (R)-Mirtazapine-d3
    		Antagonist
    (R)-Mirtazapine-d3 is a deuterium labeled (R)-Mirtazapine. (R)-Mirtazapine is a R(−)-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4[1].
    (R)-Mirtazapine-d<sub>3</sub>
  • HY-120820
    LY320954
    		Antagonist
    LY320954 is a selective 5-HT2A receptor antagonist, with a Ki of 96 nM. LY320954 potently inhibits Ca2+ influx in the functional assay (EC50 of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED50 of 4.8 mg/kg.
    LY320954
  • HY-123138
    LY206130 free base
    LY206130 free base is a 5-HT1A receptor antagonist with the activity of enhancing exogenous serotonin levels. LY206130 free base, when used concomitantly with fluoxetine, may enhance the appetite-suppressing effects of fluoxetine. LY206130 free base was shown to significantly reduce sweetened milk concentrate consumption in a dietary model. Clinical application of LY206130 free base may be beneficial in curbing eating disorders and obesity.
    LY206130 free base
  • HY-136678A
    SB 258741 hydrochloride
    		Antagonist
    SB 258741 hydrochloride is a specific 5-HT7 receptor antagonist and can be used for the research of schizophrenia.
    SB 258741 hydrochloride
  • 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-W296398
    5-Bromo-N,N-dimethyltryptamine
    		Inhibitor
    5-Bromo-N,N-dimethyltryptamine, an active metabolite, is an antidepressant and sedative drug lead. 5-Bromo-N,N-dimethyltryptamine shows strong affinity towards 5-HT1A, 5-HT2B, 5-HT6, and 5-HT7.
    5-Bromo-N,N-dimethyltryptamine
  • HY-181878
    Z8779877149
    		Ligand
    Z8779877149 (Z7149) is a blood-brain barrier-permeable multi-target ligand that targets SERT (Ki=198 nM), α2A adrenergic receptor (Ki=180 nM; EC50=440 nM) and 5-HT2A receptor (EC50=172 nM, Emax=76%). Z8779877149 inhibits 5-HT reuptake and activates Gi and Gq protein signaling pathways, respectively. Z8779877149 effectively alleviates pain responses as well as depression- and anxiety-like behaviors, while exhibiting favorable safety without inducing sedation or motor impairment. Z8779877149 is available for the research of pain, depression and anxiety disorders.
    Z8779877149
  • 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-182504
    NRA-0562
    		Modulator
    NRA‑0562 is a dopamine antagonist with high affinities for dopamine D1/D2/D3/D4, 5‑HT2A and α1‑adrenoceptors. NRA-0562 dose‑dependently reverses induced suppression of firing activity in rat A9 and A10 midbrain dopamine neurons, with preferential potency at A10 neurons (ED50 = 0.3 mg/kg). NRA-0562 elevates Fos-like immunoreactivity in rat nucleus accumbens and dorsolateral striatum. NRA-0562 can be used for preclinical research on schizophrenia..
    NRA-0562
  • HY-172339
    4-AcO-DALT hydrochloride
    		Inhibitor
    4-AcO-DALT hydrochloride is a tryptamine compound with psychoactive effects. 4-AcO-DALT hydrochloride inhibits 5-HT receptors, alpha receptors, dopamine receptors, histamine receptor 1 (H1), muscarinic M2 receptor and Sigma 2 receptor. 4-AcO-DALT hydrochloride shows Ki values of 582 nM, 2689 nM, 2099 nM, 2116 nM, 958 nM, 137 nM, 824 nM, 479 nM, 406 nM, 874 nM, 4190 nM, 482 nM, 214 nM, 803 nM, 4522 nM, 1907 nM for 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7A, H1, Sigma 2, α2A, α2B, α2C, D2, D3 receptors.
    4-AcO-DALT hydrochloride
  • HY-W777120
    Cisapride-13C,d3
    Cisapride-13C,d3 (R 51619-13C,d3) is the deuteriumand 13C-labeled Cisapride (HY-14149). Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity.
    Cisapride-<sub>13<sub>C<sub>,d<sub>3<sub>
  • HY-176910
    IHCH-7179
    		Modulator
    IHCH-7179 is a 5-HT receptor modulator. IHCH-7179 can antagonize 5-HT2A receptor and activate 5-HT1A receptor. IHCH-7179 can be used for the research of neurological disease.
    IHCH-7179
  • 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-N18471
    5,7-Dihydroxytryptamine
    		Ligand
    5,7-Dihydroxytryptamine (5,7-DHP) is an autofluorescent (λex≈365 nm), selective neurotoxin and a transport substrate for MAO-A and 5-HT. 5,7-Dihydroxytryptamine can specifically target and damage central and peripheral 5-HTergic neurons, while affecting 5-HT-related pathways and neurotransmitter balance. 5,7-Dihydroxytryptamine can be used to establish 5-HTergic neuron injury models for studies on neural development, neurodegenerative diseases, as well as mechanisms related to platelet function and retinal neurons.
    5,7-Dihydroxytryptamine
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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