Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3nM; IC50 = 0.09nM for the human receptor).It is selective for NK1 over NK3 receptors (Ki = 454.1nM for human NK3). In vivo, aprepitant (1mg/Kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P. It also reduces NK1-agonist-induced foot tapping in gerbils. Formulations containing aprepitant have been used to prevent chemotherapy-induced nausea and vomiting.
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