Neurokinin Receptors

Neurokinin receptor antagonists block the tachykinin receptors activated by substance P, neurokinin A and neurokinin B. The three subtypes, neurokinin 1, 2 and 3 receptors (NK1, NK2, NK3), are G protein-coupled receptors with different preferred ligands. Their cloning in the late 1980s began with the bovine NK2 receptor and the rat NK1 receptor. Substance P binds NK1 with the highest affinity, and this receptor is studied in emesis, pain transmission and neurogenic inflammation. Most compounds here are NK1 antagonists, including aprepitant, its phosphate prodrug fosaprepitant, rolapitant and netupitant. Ibodutant is a selective NK2 receptor antagonist used to study smooth muscle contraction in the gut.

7 Items

  • CP-96,345
    Cat. No.
    A62002

    CP-96,345

    CP-96,345 is a potent, non-peptide inhibitor targeting tachykinin and substance P receptors. This compound effectively inhibits the hypotensive effects induced by substance P and neurokinin A, making it a valuable tool for studying neurogenic inflammation. Its oral bioactivity allows for convenient application in research settings focused on pain modulation and inflammatory responses.

    1 mg
    $160.00
    5 mg
    $415.00
    All 3 sizes
  • NK3R-IN-1
    Cat. No.
    A62048

    NK3R-IN-1

    NK3R-IN-1 is a potent inhibitor of the Neurokinin Receptor NK3R, characterized as an imidazolepiperazine derivative with oral bioavailability. This compound effectively lowers blood luteinizing hormone levels in ovariectomized models, demonstrating significant influence on neuroendocrine regulation. It serves as a valuable tool for research in reproductive biology and neurobiology, particularly in studies involving hormone modulation and neurological signaling pathways.

    5 mg
    $1,125.00
    50 mg
    $2,280.00
    All 3 sizes
  • [D-Pro2,D-Phe7,D-Trp9] Substance P
    Cat. No.
    A62072

    [D-Pro2,D-Phe7,D-Trp9] Substance P

    [D-Pro2,D-Phe7,D-Trp9] Substance P is a synthetic analogue of Substance P that functions as a potent inhibitor of the neuropeptide. It exhibits a significant ability to modulate neurogenic inflammation and pain response by blocking Substance P-mediated signaling pathways. This compound is useful in studying the role of Substance P in pain and gastrointestinal motility research applications, particularly in models involving guinea-pig ileum contraction.

    Out of stock

    All 3 sizes
  • SR140333B
    Cat. No.
    A62089

    SR140333B

    SR140333B is a selective inhibitor of the neurokinin-1 (NK1) receptor, primarily involved in modulating pain and inflammatory responses. This compound demonstrates significant efficacy in reducing LPS-induced fever and attenuating LPS-induced alterations in brain tissue in rat models. SR140333B is valuable for research focusing on neuroinflammation, pain pathways, and the therapeutic potential of NK1 receptor modulation.

    25 mg
    $2,535.00
    50 mg
    $3,265.00
    All 3 sizes
  • SCH 60057
    Cat. No.
    A62103

    SCH 60057

    SCH 60057 is a potent neurokinin receptor inhibitor, selectively targeting NK1 and NK2 receptors with IC50 values of 6 μM and 12 μM, respectively. This compound is derived from Acremonium sp. and is useful in research applications related to pain modulation, inflammation, and neurogenic disorders. Its ability to inhibit neurokinin signaling pathways makes it a valuable tool for investigating the roles of these receptors in various biological processes.

    Out of stock

    All 3 sizes
  • Dilopetine citrate
    Cat. No.
    A62119

    Dilopetine citrate

    Synonyms: E-6006 citrate

    Dilopetine citrate is a potent inhibitor of substance P release, demonstrating significant activity in attenuating the vocalizations of isolated guinea pig pups in a dose-dependent manner. Its mechanisms suggest potential applications in the field of psychiatry, particularly as an antidepressant agent. This compound may facilitate research on the modulation of neuropeptide systems involved in mood regulation and pain perception.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Dazodeunetant
    Cat. No.
    A62130

    Dazodeunetant

    Dazodeunetant is a selective inhibitor of neurokinin receptors (NK), exhibiting an IC50 of 75.99 nM against NK3R in HEK293-NK3 cells. This nitrogen-containing fused ring derivative demonstrates potential in the study of menopausal hot flashes and related therapeutic strategies. Its ability to modulate neurokinin signaling positions it as a valuable tool in neurobiology and women's health research.

    Out of stock

    All 3 sizes

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