NK1 receptor antagonist

NK1 Receptor Antagonist

NK1 receptor antagonist

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Neurokinin 1 (NK<sub>1</sub>) antagonists are a novel class of medications that possesses unique antidepressant, anxiolytic, and antiemetic properties. The discovery of neurokinin 1 (NK<sub>1</sub>) 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-HT<sub>3</sub> antagonists while the delayed phase remains difficult to control. The discovery and development of NK<sub>1</sub> receptor antagonists have elicited antiemetic effect in both acute and especially in delayed phases of emesis.

The first registered clinical use of NK<sub>1</sub> receptor antagonists was the treatment of emesis, associated with cancer chemotherapy.


In 1931, von Euler and Gaddum discovered substance P in horse brain and intestine. The substance showed strong vasodilatory effects and contractile activity on the rabbit gut. A great effort was put in to 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...
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