Pharmacological Properties of a New Parasympathetic Blocking Agent, N,N Dimethyl 4-Piperidylidene 1,1 Diphenylmethane Methyl Sulfate (Prantal)

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Abstract
Prantal exhibits pharmacodynamic properties which distinguish it from previously described orally active atropine-like drugs. It selectively acts by parasympathetic blockade on gastric secretion and motility at doses which do not produce mydria-sis. By local application to the rabbit eye, 1% Prantal soln. is not mydriatic; 0.1% methantheline bromide (Banthine) produces mydriasis. In dogs, cardiac arrest by faradic vagal stimulation was blocked bv intraven. Prantal at 0.05 mg. Intraven. Prantal, 2 to 5 mg./kg., inhibited the carotid sinus pressor reflex in dogs, and blocked the faradic stimulation of the isolated superior cervical ganglion in cats. Orally, 37.5 mg/kg. of Prantal inhibited gastric motility in dogs as effectively as 75 mg/kg- of methantheline bromide when measured by roentgenologic determination of gastric emptying time after a BaSO4 meal. In these tests methantheline bromide produced mydriasis which persisted for 1 to 2 hrs; Prantal was not mydriatic. In other expts, gastric secretion volume during intraven. infusion of histamine diHCl (0.1 mg. /kg./hr.) was reduced 50 to 90% by intraven. Prantal at 1 mg./kg. and titratable total acid was decreased 44-97%. Clinical findings in man are reported which confirm the gastric antispasmodic action, and the reduction in volume and acidity of gastric secretion at dosages which rarely produce mydriasis or xerostomia.