いわゆる"Antiphobic Drug" Pipethanateの新誘導体(PI-3610-T)の薬理作用(<特集>脳と神経の研究II)

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A new derivative of pipethanate, 2-piperidinoethyl benzilate-N-methyl-p-toluerie sulfonate (PI-3610-T) produces a mydriatic effect in rabbits, cats and other species. The effects of PI-3610-T have been studied. 1) Doses of PI-3610-T less than 10 mg/kg exhibit no sedative effects in mice (i. p.), rabbits (i. v.), cats (i. p.) or monkeys (p. o.). Slight sedation is observed only with administration of larger amounts of the drug. 2) Doses of 2.5 and 5 mg/kg (i. v.) of PI-3610-T produce a transient fall in blood pressure in rabbits and cats; the agent has marked cholinolytic properties, but no adrenolytic actions. The hypotensive effect of PI-3610-T is not altered by high spinal cord transection, vagotomy or atropiriization. Further, it produces little or no direct depressant effects on the heart. 3) The cholinolytic potency of PI-3610-T is approximately the same or less than that of atropine on the frog rectus muscle, isolated guinea pig ileum or the gastrointestinal tract of mice in vivo. 4) PI-3610-T displays competitive ganglionic blocking properties as measured on the postganglionic potentials of the superior cervical ganglion and in spontaneous discharges of the inferior mesenteric ganglion of the cat. 5) Segmental spinal cprd reflex potentials of cats are suppressed by PI-3610-T in anesthetized preparations, but not in the spinal cats. 6) PI-3610-T (≤10 mg/kg i. v.) does not inhibit neuromuscular transmission in rabbit's sciatic nerve-gastrocnemius muscle preparation. 7) Instillation of 1% solution of PI-3610-T produces remarkable pupillary dilatation in rabbits, cats and other species. The combination of marked mydriatic action on local application and low systemic toxity suggests it for clinical trials.
千葉大学の論文
1965-11-28

いわゆる"Antiphobic Drug" Pipethanateの新誘導体(PI-3610-T)の薬理作用(<特集>脳と神経の研究II)

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