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casopitant mesylate The mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. Casopitant competitively binds to and blocks the activity of the NK1 receptor, thereby inhibiting NK1-receptor binding of the endogenous tachykinin neuropeptide substance P (SP), which may result in antiemetic effects. SP is found in neurons of vagal afferent fibers innervating the brain-stem nucleus tractus solitarii and the area postrema, which contains the chemoreceptor trigger zone (CTZ), and may be elevated in response to chemotherapy. The NK1 receptor is a G-protein receptor coupled to the inositol phosphate signal-transduction pathway and is found in both the nucleus tractus solitarii and the area postrema. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
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Synonym: | ![](https://webarchive.library.unt.edu/eot2008/20090115054802im_/http://www.cancer.gov/images/spacer.gif) | casopitant | | ![](https://webarchive.library.unt.edu/eot2008/20090115054802im_/http://www.cancer.gov/images/spacer.gif) | Code name: | ![](https://webarchive.library.unt.edu/eot2008/20090115054802im_/http://www.cancer.gov/images/spacer.gif) | GW679769 | | ![](https://webarchive.library.unt.edu/eot2008/20090115054802im_/http://www.cancer.gov/images/spacer.gif) |
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