Rolapitant (SCH 619734): A potent, selective and orally active neurokinin NK1 receptor antagonist with centrally-mediated antiemetic effects in ferrets

►Rolapitant (SCH 619734) is a high affinity, selective, neurokinin NK1 functional antagonist. ►SCH 619734 penetrates the central nervous system following oral administration. ►SCH 619734 dose-dependently inhibits NK1 receptor-mediated foot tapping in gerbils. ►Rolapitant reverses both apomorphine and cisplatin-induced emesis in ferrets.