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一系列双季铵托品碱的神经肌肉阻滞特性

The neuromuscular blocking properties of a series of bis-quaternary tropeines.

作者信息

HAINING C G, JOHNSTON R G, SMITH J M

出版信息

Br J Pharmacol Chemother. 1960 Mar;15(1):71-81. doi: 10.1111/j.1476-5381.1960.tb01212.x.

Abstract

Linkage of two tropine esters through their nitrogen atoms by the chain -CH(2)-O-CO-CH(2)-CO-O-CH(2)-, in which m was 2 or 3 and n varied from 0 to 6, gave compounds which produced neuromuscular block without depolarization. Reversibility be neostigmine was confirmed for a few compounds. Potency was found to depend upon the tropine ester employed and upon the values of n and m. Short duration and hypotensive properties were favoured by the higher values of n. The duration of action of the compound based on the phenylacetic acid ester of tropine, in which n=4 and m=2, varied considerably in different species. Epimerization, in which the relative positions of the methyl group and the linking chain on the quaternary tropane nitrogen atom were reversed, did not produce subtances having more favourable properties than those possessed by the unepimerized compounds.

摘要

通过链-[CH₂]ₘ-O-CO-[CH₂]ₙ-CO-O-[CH₂]ₘ-将两个托品酯通过它们的氮原子连接起来,其中m为2或3,n从0到6变化,得到了产生非去极化神经肌肉阻滞的化合物。对一些化合物证实了新斯的明可使其逆转。发现效力取决于所使用的托品酯以及n和m的值。n值较高有利于作用持续时间短和具有降压特性。基于托品苯乙酸酯的化合物(其中n = 4且m = 2)在不同物种中的作用持续时间有很大差异。差向异构化,即四级托烷氮原子上甲基和连接链的相对位置颠倒,并未产生比未差向异构化的化合物具有更有利性质的物质。

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