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Tachykinin receptors are a family of G protein-coupled receptors (GPCRs) that bind tachykinin neuropeptides, leading to various physiological responses such as smooth muscle contraction, vasodilation, and modulation of neurotransmitter release. There are three main mammalian tachykinin receptors: NK1, NK2, and NK3. Upon ligand binding, the receptor activates Gq/11 proteins, leading to activation of phospholipase C and subsequent mobilization of intracellular calcium stores and activation of protein kinase C. Antagonists targeting especially the NK1 receptor have been developed for clinical use, primarily for chemotherapy-induced nausea/vomiting.
Antagonism of tachykinin receptors, primarily NK1
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