Neurokinin Type 1 Receptor (NK1R)

The Neurokinin Type 1 Receptor (NK1R), also known as TACR1 or Substance P Receptor, is a G protein-coupled receptor belonging to the tachykinin receptor subfamily. It is activated primarily by the neuropeptide substance P (SP) and plays a crucial role in various physiological processes, including pain transmission, stress response, emesis, vasodilation, and immune modulation. NK1R is widely distributed throughout the central and peripheral nervous systems and peripheral tissues. Antagonists targeting NK1R, such as aprepitant, are used as antiemetics to prevent chemotherapy-induced nausea and vomiting. Research is ongoing to explore their potential use in treating mood disorders and cancer.

Other names

Tachykinin receptor 1TACR1Substance P receptorSPR

NK1R antagonists bind to and block the neurokinin 1 receptor, preventing substance P from binding and activating the receptor. This inhibits downstream signaling pathways, including activation of phospholipase Cβ and increased intracellular calcium concentration.