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仲烷氧基烷基氨基酰苯胺的合成及其局部麻醉特性

Synthesis and local anesthetic properties of secondary alkoxyalkylaminoacylanilides.

作者信息

Kronberg G H, Leard R S, Meymaris E, Takman B H

出版信息

J Pharm Sci. 1978 May;67(5):595-600. doi: 10.1002/jps.2600670505.

Abstract

Nineteen secondary alkoxyalkylaminoacylanilides were prepared. They were weaker bases and were more hydrophilic than the corresponding analogs lacking the ether function. In 2% solution, these compounds blocked the rat sciatic nerve in vivo after relatively short onset times with good frequency of anesthesia. The duration of block was 0.4--1.5 times that of lidocaine. Their systemic toxicity was low, and their irritation liability in most instances was acceptable.

摘要

制备了19种仲烷氧基烷基氨基酰苯胺。它们是较弱的碱,并且比缺乏醚功能的相应类似物更具亲水性。在2%的溶液中,这些化合物在体内阻断大鼠坐骨神经的起效时间相对较短,麻醉频率良好。阻断持续时间为利多卡因的0.4 - 1.5倍。它们的全身毒性较低,在大多数情况下其刺激性是可以接受的。

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