Neurokinin 1 receptor, Neurokinin 2 receptor, Neurokinin 3 receptor (NK1R, NK2R, NK3R)

Neurokinin 1 receptor (NK1R), Neurokinin 2 receptor (NK2R), and Neurokinin 3 receptor (NK3R) are members of the tachykinin receptor family of G protein-coupled receptors (GPCRs) that bind different tachykinin neuropeptides, namely substance P (NK1R), neurokinin A (NK2R), and neurokinin B (NK3R)[1][2][3][5]. These receptors mediate diverse physiological effects, including signal transduction in the nervous system, modulation of pain (nociception), emesis, inflammation, stress, mood disorders, smooth muscle contraction, and the regulation of the reproductive axis (notably by NK3R)[1][2][3][4][5]. They are important therapeutic targets, particularly NK1R, for which several antagonists are approved for the management of chemotherapy-induced nausea and vomiting[3][4][5]. Antagonists and agonists targeting this receptor family continue to be studied for broader applications, including depression, pain, and gastrointestinal disorders[3][4].

Other names

NK1R (for Neurokinin 1 receptor)NK2R (for Neurokinin 2 receptor)NK3R (for Neurokinin 3 receptor)Substance P receptor (for NK1R)[5]TACR1 (gene for NK1R)[5]Tachykinin receptor 1Tachykinin receptor 2Tachykinin receptor 3

Receptor antagonism (blockade of neurokinin receptor, e.g., NK1R antagonists such as aprepitant for antiemetic action)[3][4]; Receptor agonism (e.g., senktide as a synthetic NK3R agonist)[1][2]; Modulation of G protein signaling (downstream effects on cAMP, phospholipase C, Ca²⁺ mobilization)[1][2][3]