Substance-P receptor (Neurokinin 1 receptor) (NK1R)

The Human neurokinin 1 receptor (NK1R), also known as the substance P receptor, is a member of the G protein-coupled receptor (GPCR) superfamily and the primary target for the tachykinin neuropeptide substance P [3, 6]. It is widely expressed in the central nervous system, particularly in regions like the area postrema and nucleus tractus solitarius, where it plays a critical role in the emetic reflex [1, 7]. Beyond its role in nausea and vomiting, NK1R is involved in pain transmission, mood regulation, and neurogenic inflammation [5, 8]. In clinical practice, NK1R antagonists such as aprepitant are standard-of-care treatments for preventing chemotherapy-induced nausea and vomiting (CINV) [2, 4]. Research also explores its potential as a therapeutic target in oncology, where its overexpression is linked to tumor cell proliferation and metastasis, as well as in psychiatric and inflammatory disorders [9, 14, 15].

Other names

TACR1NK1RSPRNK-1 receptorTachykinin receptor 1Substance P receptor

Competitive antagonism of the neurokinin 1 receptor, which blocks the binding of the endogenous ligand substance P and inhibits downstream signaling pathways such as the Gq/11-mediated activation of phospholipase C [1, 8].