NK1 receptor antagonist

Neurokinin 1 (NK₁) antagonists are a novel class of medications that possesses unique antidepressant,anxiolytic, and antiemetic properties. The discovery of neurokinin 1 (NK₁) receptor antagonists was a turning point in the prevention of nausea and vomiting associated with cancer chemotherapy.

An example of a drug in this class is aprepitant. Chemotherapy-induced emesis appears to consist of acute and delayed phases. So far, the acute phase emesis responds to 5-HT₃ antagonists while the delayed phase remains difficult to control. The discovery and development of NK₁ receptor antagonists have elicited antiemetic effect in both acute and especially in delayed phases of emesis. Casopitant, netupitant and rolapitant are some newer additions in this group. Rolapitant has a significantly long half life of 160 hours and got approval by the USFDA in 2015.

The first registered clinical use of NK₁ receptor antagonists was the treatment of emesis, associated with cancer chemotherapy.

In 1931, von Euler and Gaddum discovered substance P (SP) in horse brain and intestine. The substance showed strong vasodilatory effects and contractile activity on the rabbit gut. A great effort was put into purifying this substance from diverse mammalian tissue, but 30 years of research were without success. Nonmammalian peptides that elicited the same vasodilatory and contractile effects as SP were discovered by Erspamer in the early 1960s. These peptides had a common C-terminal sequence, and were grouped together as tachykinins. In 1971, Chang managed to purify SP from horse intestine and identify its amino acid sequence; SP was then classified as a mammalian tachykinin. Later it became clear that SP was a neuropeptide that was common in the central and peripheral nervous system. In the mid 1980s, the additional mammalian tachykinin neurokinin A (NKA) and neurokinin B (NKB) were discovered. This led to further research, resulting in the isolation of the genes that encoded the mammalian tachykinins and eventually the discovery of three different tachykinin receptors. In 1984, it was decided that the tachykinin receptors should be called tachykinin NK₁ receptor, tachykinin NK₂ receptor and tachykinin NK₃ receptor.

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