产品描述:
Rolapitant is a potent neurokinin-1 (NK1) receptor antagonist (Ki = 0.66 nM for the human receptor).{35201} It is greater than 1,000-fold selective for NK1 over NK2 and NK3 and lacks activity in a panel of 100 receptors, transporters, enzymes, and ion channels. Rolapitant inhibits GR-73632-induced calcium efflux in CHO cells expressing human NK1 in a concentration-dependent manner. In vivo, rolapitant inhibits GR-73632-induced foot-tapping in gerbils (ID90 = 0.3 mg/kg). It also prevents emesis in ferrets induced by apomorphine (Item No. 16094) and cisplatin (Item No. 13119) with ED50 values of 0.03 and 0.07 mg/kg, respectively. Formulations containing rolapitant have been used to prevent chemotherapy-induced nausea and vomiting.