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.

3 Items

  • Eprazinone dihydrochloride
    Cat. No.
    A16529

    Eprazinone dihydrochloride

    Eprazinone dihydrochloride is a selective neurokinin 1 receptor (NK1R) ligand known for its mucolytic, secretolytic, antitussive, and bronchial antispasmodic properties. It exhibits significant potential in the treatment of chronic bronchitis, contributing to enhanced pulmonary function and improved arterial partial pressure of oxygen. This compound is valuable in research applications focused on respiratory disorders and the modulation of NK1 receptor pathways.

    50 mg
    $20.00
    100 mg
    $25.00
    All 4 sizes
  • Leucyl-phenylalanine amide
    Cat. No.
    A62091

    Leucyl-phenylalanine amide

    Synonyms: L-Leucyl-L-phenylalaninamide

    Leucyl-phenylalanine amide is a dipeptide analog that serves as a specific ligand for the SP1-7 receptor, exhibiting a binding affinity characterized by a Ki value of 10.2 nM. This compound is valuable for research focused on neuropeptide signaling pathways and can be utilized in studies exploring the functional roles of SP1-7 in various physiological contexts. Notably, it does not show binding activity to human NK-1 or NK-3 receptors, making it a selective tool for targeted biological investigations.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes
  • Phenylalanylphenylalanylamide
    Cat. No.
    A62120

    Phenylalanylphenylalanylamide

    Synonyms: H-Phe-Phe-NH2

    Phenylalanylphenylalanylamide (H-Phe-Phe-NH₂) functions as a potent ligand for the substance P 1–7 (SP1-7) binding site, exhibiting a Ki value of 1.5 nM. This compound demonstrates significant anti-allodynic and anti-hyperalgesic properties in animal models of neuropathic pain when administered centrally. However, it shows no distinct effects when delivered peripherally via intraperitoneal injection. Phenylalanylphenylalanylamide is valuable for investigations into pain-related disorders and therapeutic interventions.

    25 mg
    $1,275.00
    50 mg
    $1,625.00
    All 3 sizes

3 Items

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