1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-169791
    ECPLA
    Agonist
    ECPLA, a lysergamide lysergic acid diethylamidean (LSD) analog, is a potent 5-HT2A agonist (EC50 of 14.6 nM) for Gq-mediated calcium flux. ECPLA has high affinity for most serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors.
    ECPLA
  • HY-103139
    Altanserin hydrochloride
    Ligand
    Altanserin is a 5-hydroxytryptamine (5-HT2A ) selective radioligand. Altanserin delivers human serotonin. Altanserin can be used to study the biochemical and cellular mechanisms of vulnerability to extracellular 5-HT increase .
    Altanserin hydrochloride
  • HY-A0095S
    Flibanserin-d4
    Modulator
    Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM).
    Flibanserin-d<sub>4</sub>
  • HY-19417
    Wf-516 hydrochloride
    Antagonist
    Wf-516 hydrochloride is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively.Wf-516 hydrochloride has potent antidepressant activity.
    Wf-516 hydrochloride
  • HY-B0002BS1
    Ondansetron-d3
    Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy.
    Ondansetron-d<sub>3</sub>
  • HY-124412
    Paynantheine
    Agonist
    Paynantheine is an alkaloid with antinociceptive activity, which is found in Mitragyna speciosa. Paynantheine is also a 5-HT1AR and 5-HT2BR agonist that induces lower lip retraction and antinociception in rats.
    Paynantheine
  • HY-171235
    5-HT2A antagonist 3
    Antagonist
    5-HT2A antagonist 3 (Formula (III)) is a 5-HT2A receptor antagonist and inverse agonist with a pIC50 of 8.7 and a pKi of 9. 5-HT2A antagonist 3 can be utilized in neurological reesearch.
    5-HT2A antagonist 3
  • HY-122303
    4-hydroxy DiPT hydrochloride
    Agonist 99.9%
    4-hydroxy DiPT hydrochloride is an 5-HT2A agonist that induces the head-twitch response (HTR) in mice, indicating psychoactivity. 4-hydroxy DiPT hydrochloride significantly reduced freezing responses to conditioned cues in a dose-dependent manner with a greater potency in female mice than male mice.
    4-hydroxy DiPT hydrochloride
  • HY-103115
    Pruvanserin hydrochloride
    Antagonist
    Pruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT2A receptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2A receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia.
    Pruvanserin hydrochloride
  • HY-101208A
    L-694247 TFA
    Agonist
    L694247 (TFA) is a selective 5-HT1D agonist with pIC50 values of 10.03, 8.64, 6.42, and 5.66 for 5-HT1D, 5-HT1A, 5-HT1C, and 5-HT1E receptors, respectively.
    L-694247 TFA
  • HY-156534
    5-HT2A&5-HT2C agonist-1
    Agonist
    5-HT2A&5-HT2C agonist-1 (Example 2) is a 5-HT2A & 5-HT2C agonist, with IC50s of 196 nM and 0.9 nM respectively. 5-HT2A&5-HT2C agonist-1 can be used for research of depression, alcoholism, tobacco and cocaine addiction, inflammation, cluster headache, PTSD, seizure disorders and other CNS disorders.
    5-HT2A&5-HT2C agonist-1
  • HY-W719093
    Citalopram hydrochloride
    Inhibitor
    Citalopram hydrochloride is an orally active 5-HT Receptor inhibitor. Citalopram hydrochloride can be used in depression research.
    Citalopram hydrochloride
  • HY-125784A
    (R)-Viloxazine hydrochloride
    Modulator 99.08%
    (R)-Viloxazine hydrochloride is a less active R-isomer of Viloxazine hydrochloride. Viloxazine hydrochloride is an effective antidepressant agent.
    (R)-Viloxazine hydrochloride
  • HY-19297
    SB-247853
    Antagonist
    SB-247853 is a highly specific 5-HT2c receptor antagonist. SB-247853 induces orthostatic intolerance during head-up tilting. SB-247853 can be used in the research of cardiovascular diseases.
    SB-247853
  • HY-175194
    5-HT2C agonist-6
    Agonist
    5-HT2C agonist-6 (Compound 13), a tricyclic psychedelic psychoplastogen, is a 5-HT2C agonist with an EC50 of 13.8  nM. 5-HT2C agonist-6 can be used for neurological diseases research.
    5-HT2C agonist-6
  • HY-B0750S1
    Dolasetron-d5
    Antagonist
    Dolasetron (MDL-73147)-d5 is deuterated labeled Dolasetron (HY-B0750). Dolasetron is a serotonin 5-HT3 receptor antagonist. Dolasetron acts as an antiemetics agent and can be used for the research of chemotherapy-induced nausea and vomiting in cancer.
    Dolasetron-d<sub>5</sub>
  • HY-172678
    PUC-10
    Antagonist
    PUC-10 is a 5-HT6 receptor antagonist with a Ki of 14.6 nM and an IC50 of 32 nM. In silico predictions suggest that PUC-10 is orally active and can cross the blood-brain barrier. PUC-10 can induce autophagy in SH-SY5Y cells by inhibiting the mTOR pathway. PUC-10 can be used in the research of neurological disorders.
    PUC-10
  • HY-106522
    Iprazochrome
    Antagonist
    Iprazochrome is a serotonin antagonist. Iprazochrome can be used in prophylaxis of migraine.
    Iprazochrome
  • HY-167677
    ASP-2205
    Agonist
    ASP-2205 is a 5-HT2C receptor agonist (human 5-HT2C receptor, EC50=0.85 nM; rat 5-HT2C receptor, EC50=2.5 nM). ASP-2205 enhances the pudendal nerve-mediated urethral closure reflex through the 5-HT2C receptor, thereby preventing urinary incontinence.
    ASP-2205
  • HY-W716520
    Cariprazine-d8
    Cariprazine-d8-1 (RGH-188-d8-1) is the deuterium labeled Cariprazine (HY-14763). Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
    Cariprazine-d<sub>8</sub>
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