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普萘洛尔对5-羟色胺神经节兴奋作用的拮抗作用。

Antagonism by propranolol of the ganglion stimulant action of 5-hydroxytryptamine.

作者信息

Weinstock M, Schechter Y

出版信息

Eur J Pharmacol. 1975 Jun-Jul;32(02):293-301. doi: 10.1016/0014-2999(75)90296-4.

Abstract

The effects of racemic propranolol and its constituent isomers were studied on ganglionic stimulation produced in situ by close arterial injection of 5-HT and DMPP to the superior cervical ganglion. Ganglion stimulation was recorded in terms of the resultant contraction of the nictitating membrane. d,l-Propranolol caused a biphasic antagonism of the ganglion stimulant effect of 5-HT. At low doses, 0.5-10 mug, the antagonism was surmountable by increasing the amount of 5-HT. The l-isomer (0.2-4 mug) but not d-propranolol also caused antagonism. At higher doses, 0.1-5 mg, both d,l- and d-propranolol caused a second type of blockade of 5-HT which was not surmountable and resembled that seen with procaine. The ganglion stimulant effects of DMPP and acetylcholine were only antagonised by the higher doses of d- and d,l-propranolol. d,l-Propranolol did not reduce the direct stimulation by 5-HT on the muscle of the nictitating membrane.

摘要

研究了消旋普萘洛尔及其组成异构体对通过向上颈神经节近距离动脉注射5-羟色胺(5-HT)和二甲基苯基哌嗪(DMPP)在原位产生的神经节刺激的影响。根据瞬膜的收缩情况记录神经节刺激。消旋普萘洛尔对5-HT的神经节兴奋作用产生双相拮抗作用。在低剂量(0.5-10微克)时,通过增加5-HT的量可克服这种拮抗作用。左旋异构体(0.2-4微克)可产生拮抗作用,而右旋普萘洛尔则不能。在高剂量(0.1-5毫克)时,消旋普萘洛尔和右旋普萘洛尔均对5-HT产生第二种类型的阻断作用,这种阻断作用不可克服,类似于普鲁卡因所见的情况。DMPP和乙酰胆碱的神经节兴奋作用仅被高剂量的右旋和消旋普萘洛尔所拮抗。消旋普萘洛尔不降低5-HT对瞬膜肌肉的直接刺激作用。

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