Casopitant

  • Chemical Properties
CAS No. 414910-27-3 Cat. No. BCP18249
Name Casopitant
Synonyms GW679769; GW 679769; GW-679769;
Formula C30H35F7N4O2 M. Wt 616.62
  • Biological Activity
Description Casopitant is a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities. Casopitant competitively binds to and blocks the activity of the NK-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 NK-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.
Pathways Neuro Signaling Pathway GPCR/G Protein 
Targets NK Receptor 

Structure

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