RT Journal Article SR Electronic T1 OBSERVATIONS ON THE PHARMACOLOGY OF DIPHENIDOL, A POTENT ANTIEMETIC JF Journal of Pharmacology and Experimental Therapeutics JO J Pharmacol Exp Ther FD American Society for Pharmacology and Experimental Therapeutics SP 339 OP 345 VO 154 IS 2 A1 Charles A. Leonard A1 Tsuneo Fujita A1 David H. Tedeschi A1 Charles L. Zirkle A1 Edwin J. Fellows YR 1966 UL http://jpet.aspetjournals.org/content/154/2/339.abstract AB Pharmacologic actions of diphenidol (α, α-diphenyl-1-piperidinebutanol, SK&F 478) and chlorpromazine were compared in animals. Although both drugs protect dogs against apomorphine-induced emesis, diphenidol does not depress motor activity at antiemetic doses and has a greater separation between the antiapomorphine ED50 and doses producing overt effects. In rats, unlike chlorpromazine, diphenidol neither blocks the conditioned escape response nor prolongs the duration of ether-induced prostration. Diphenidol is less potent than chlorpromazine in depressing motor activity of mice and in prolonging the duration of pentobarbital-induced prostration in rats. Diphenidol has no significant antihistamine activity in guinea pigs and does not alter the rate at which charcoal passes through rat intestine. In unanesthetized dogs, at oral doses 6 times the antiapomorphine ED50, diphenidol has no significant effect upon blood pressure, heart rate, respiration rate and electrocardiogram. In anesthetized dogs at intravenous doses up to 10 times the oral antiapomorphine ED50, diphenidol produces weak anticholinergic effects in the order of 1/330 the potency of atropine. The animal tests show that diphenidol is equal in antiapomorphine potency to chlorpromazine and that diphenidol has a greater selectivity of pharmacologic action. Clinical tests show good correlation with the laboratory observations and demonstrate that diphenidol is indeed an effective antiemetic agent in man. © 1966 by The Williams & Wilkins Company