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对一种新型抗心律失常药物ORG 6001进行特性研究,包括一项简单的钙拮抗试验。

Investigations to characterize a new anti-arrhythmic drug, ORG 6001 including a simple test for calcium antagonism.

作者信息

Salako L A, Williams V, Wittig J H

出版信息

Br J Pharmacol. 1976 Jun;57(2):251-62. doi: 10.1111/j.1476-5381.1976.tb07475.x.

Abstract

1 The compound Org 6001 (3alpha-amino-2beta-hydroxy-5alpha-androstan-17-one hydrochloride) was found in recent experiments to exhibit anti-arrhythmic activity. Evidence is presented in this paper concerning its mode of action. 2 Org 6001 was 1.8 times more potent than procaine as a local anaesthetic on desheathed frog nerve. 3 Org 6001 had no effect on the resting potential of isolated cardiac muscle of rabbit, but greatly reduced the maximum rate of depolarization tion (MRD). The action potential duration TAPD) WAS MARGINALLY PROLONGED IN ATRIAL AND VENTRICULAR MUSCLE. 4 Org 6001 preferentially shortened APD in that part of the Purkinje system in which APD is normally longer than elsewhere, so that APD

摘要
  1. 化合物Org 6001(3α-氨基-2β-羟基-5α-雄甾烷-17-酮盐酸盐)在最近的实验中被发现具有抗心律失常活性。本文提供了有关其作用方式的证据。2. Org 6001作为局部麻醉剂对去鞘青蛙神经的效力比普鲁卡因高1.8倍。3. Org 6001对兔离体心肌的静息电位没有影响,但大大降低了最大去极化速率(MRD)。心房和心室肌的动作电位持续时间(TAPD)略有延长。4. Org 6001优先缩短浦肯野系统中动作电位时程(APD)通常比其他部位更长的那部分的APD,从而使APD……(原文此处不完整)

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Heart: excitation and contraction.心脏:兴奋与收缩。
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