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一些神经肌肉阻滞药物在体内和体外的相对效价。

Relative potency of some neuromuscular blocking drugs in vivo and in vitro.

作者信息

Anttila P, Ertama P

出版信息

Med Biol. 1978 Jun;56(3):152-5.

PMID:682698
Abstract

The relative potencies of alcuronium, d-tubocurarine, gallamine, pancuronium and succinylcholine as neuromuscular blocking agents were tested in vivo (acute toxicity in mice) and in vitro (rat phrenic nerve-diaphragm preparation). In vivo, pancuronium was about 4 times more potent than alcuronium or d-tubocurarine, whose LD50-values were of the order of 2 X 10(-7) mol/kg. On a molar basis, succinylcholine was about 5 times less potent and gallamine about 20 times less potent than alcuronium or d-tubocurarine. In vitro, succinylcholine was as effective as d-tubocurarine and alcuronium. The IC50-values for these drugs were of the drugs were of the order of 2 X 10(-6)M. Pancuronium was about 2 times less potent and gallamine about 100 times less potent than the other three drugs in vitro. The in vivo-potencies correlate better than those obtained in vitro with observations from the clinical use of these muscle relaxants.

摘要

在体内(小鼠急性毒性实验)和体外(大鼠膈神经 - 膈肌标本)测试了阿库氯铵、右旋筒箭毒碱、加拉明、泮库溴铵和琥珀酰胆碱作为神经肌肉阻滞剂的相对效价。在体内,泮库溴铵的效价约为阿库氯铵或右旋筒箭毒碱的4倍,它们的半数致死量(LD50)值约为2×10⁻⁷mol/kg。以摩尔为基础,琥珀酰胆碱的效价比阿库氯铵或右旋筒箭毒碱约低5倍,加拉明约低20倍。在体外,琥珀酰胆碱与右旋筒箭毒碱和阿库氯铵的效果相当。这些药物的半数抑制浓度(IC50)值约为2×10⁻⁶M。在体外,泮库溴铵的效价比其他三种药物约低2倍,加拉明约低100倍。与这些肌肉松弛剂临床应用的观察结果相比,体内效价比体外效价的相关性更好。

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