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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.
Synonyms: Eledoisin RP
Eledoisin Related Peptide is a neurokinin receptor activator that functions as an analog of Substance P. This peptide is known to stimulate neurons, resulting in various behavioral responses. It serves as a valuable tool for research applications focused on neurokinin signaling pathways and tachykinin receptor interactions.
