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-106157A
    Donitriptan mesylate
    Agonist
    Donitriptan Mesylate is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
    Donitriptan mesylate
  • HY-19358B
    2-Methyl-5-HT maleate
    Agonist
    2-Methyl-5-HT maleate (2-Methyl-5-hydroxytryptamine maleate) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT maleate is shown to display anti-depressive-like effects.
    2-Methyl-5-HT maleate
  • HY-146232
    F 13714
    Agonist
    F 13714 (F 14679) is a prototypical 5-HT1A agonist with a pKi of 10.23. F 13714 induces large Ca2+ responses.
    F 13714
  • HY-121574
    RU 27849
    Agonist
    RU 27849 (Compound 27) is a 5-HT receptor 2A agonist, and can be used to study tryptamine recognition site binding.
    RU 27849
  • HY-106964A
    (Rac)-S 16924
    Agonist
    (Rac)-S 16924 is a partial agonist of the 5-HT1A receptor. (Rac)-S 16924 regulates signaling through its interaction with the 5-HT1A receptor, and (Rac)-S 16924 can stabilize the receptor in its G-protein-coupled conformation without fully activating it, which may affect intracellular signaling pathways associated with this receptor. (Rac)-S 16924 can be used to study the 5-HT1A receptor in mental disorders, especially schizophrenia.
    (Rac)-S 16924
  • HY-B0031S2
    Quetiapine-d8 fumarate
    Agonist
    Quetiapine-d8 (fumarate) is the deuterium labeled Quetiapine. Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine 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>8</sub> fumarate
  • HY-W713312
    2,6-DMA hydrochloride
    Agonist
    2,6-DMA hydrochloride is classified as an amphetamine. 2,6-DMA hydrochloride is a serotonin 5-HT2 receptor agonist with an apparent pA2 value of 5.09.
    2,6-DMA hydrochloride
  • HY-123747A
    SC-53116 hydrochloride
    Agonist
    SC-53116 hydrochloride is a selective 5-HT4 receptor agonist with EC50 at 23 nM.
    SC-53116 hydrochloride
  • HY-111985
    Revospirone
    Agonist
    Revospirone (BAY Vq 7813) is a partial agonist of the 5-HT1A receptor with a Ki of 2 nmol/L. Revospirone inhibits adenylate cyclase activity with an IC50 of 124 nmol/L.
    Revospirone
  • HY-169785
    7-Methyl DMT
    Agonist
    7-Methyl DMT (7-TMT) is a 5-HT2 receptor agonist. Structurally, 7-Methyl DMT is a tryptamine derivative. It can be used as an analytical reference standard for the psychoactive substance DOM. 7-Methyl DMT is also used in research in the field of neurological diseases.
    7-Methyl DMT
  • HY-100166R
    AP521 (Standard)
    Agonist
    AP521 (Standard) is the analytical standard of AP521 (HY-100166). This product is intended for research and analytical applications. AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
    AP521 (Standard)
  • HY-102057R
    Felcisetrag (Standard)
    Agonist
    Felcisetrag (Standard) is the analytical standard of Felcisetrag (HY-102057). This product is intended for research and analytical applications. Felcisetrag (TD-8954) is an orally active, potent and selective 5-HT4 receptor agonist with gastrointestinal prokinetic properties. Felcisetrag has high affinity (pKi =9.4) for human 5-HT4(c) receptors.
    Felcisetrag (Standard)
  • HY-116065
    CUMI-101
    Agonist
    CUMI-101 (compound 8) is a 5-HT1AR agonist (Ki=0.15 nM) with an EC50 of 0.1 nM in the [35S]GTPγS binding assay. CUMI-101 can be used in the research of neurological diseases.
    CUMI-101
  • HY-103142R
    AS19 (Standard)
    Agonist
    AS19 (Standard) is the analytical standard of AS19 (HY-103142). This product is intended for research and analytical applications. AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.
    AS19 (Standard)
  • HY-W740014
    N-Desmethyl Zolmitriptan
    Agonist
    N-Desmethyl Zolmitriptan (183C91; DZT) is the active metabolite of the serotonin (5-HT) receptor subtype 5-HT1B and 5-HT1D agonist Zolmitriptan (HY-B0229). N-Desmethyl Zolmitriptan (183C91; DZT) is an agonist of 5-HT1B receptors and induces constriction in isolated human cerebral arteries (EC50=100 nM).
    N-Desmethyl Zolmitriptan
  • HY-10457AR
    Velusetrag hydrochloride (Standard)
    Agonist
    Velusetrag hydrochloride (Standard) is the analytical standard of Velusetrag hydrochloride (HY-10457A). This product is intended for research and analytical applications. Velusetrag (TD-5108) hydrochloride is an orally active, potent and selective agonist of serotonin 5-HT4 receptor (5-HT4R), with a pKi of 7.7. Velusetrag hydrochloride exhibits no affinity (Ki>10 μM) for 5-HT2A and 5-HT2B receptors. Velusetrag hydrochloride can be used for the research of gastrointestinal diseases and Parkinson's disease.
    Velusetrag hydrochloride (Standard)
  • HY-B0189AR
    Mosapride citrate (Standard)
    Agonist
    Mosapride (citrate) (Standard) is the analytical standard of Mosapride (citrate). This product is intended for research and analytical applications. Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases.
    Mosapride citrate (Standard)
  • HY-119820
    Xaliproden free base
    Agonist
    Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety.
    Xaliproden free base
  • HY-16688R
    RU 24969 (Standard)
    Agonist
    RU 24969 (Standard) is the analytical standard of RU 24969. This product is intended for research and analytical applications. RU 24969 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 could decrease fluid consumption and increase forward locomotion.
    RU 24969 (Standard)
  • HY-W708033
    25E-NBOMe hydrochloride
    Agonist 99.9%
    25E-NBOMe hydrochloride is a derivative of 2C-E having an N-(2-methoxybenzyl) addition at the amine. 25E-NBOMe hydrochloride is a selective /b>5-HT2A receptor agonist.
    25E-NBOMe hydrochloride
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