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局部麻醉药:2-N,N-二烷基氨基酰基-2'-甲基(或2',6'-二甲基)-4'-丁基氨基苯胺

Local anesthetics: 2-N,N-dialkylaminoacyl-2'-methyl (or 2',6'-dimethyl)-4'-butylaminoanilides.

作者信息

Foye W O, Jan C M, Takman B H

出版信息

J Pharm Sci. 1982 Jun;71(6):680-6. doi: 10.1002/jps.2600710619.

Abstract

A series of tetracaine analogs based on the lidocaine structure, having a 2'-methyl-(or 2',6'-dimethyl)-4-butylaminoanilide moiety with alpha substitution on the dialkylaminoacyl function, has been synthesized. Local anesthetic activity was found with the N-butyl derivatives in both the 2'-methyl and 2',6'-dimethyl series using both the method of rabbit cornea loss of reflex and spinal anesthesia in sheep. Duration of activity of the compounds was greater than that of lidocaine, but less than that of tetracaine, with comparable dosage levels.

摘要

已合成了一系列基于利多卡因结构的丁卡因类似物,其具有2'-甲基-(或2',6'-二甲基)-4-丁基氨基苯甲酰部分,在二烷基氨基酰官能团上有α取代基。使用兔角膜反射消失法和绵羊脊髓麻醉法,在2'-甲基和2',6'-二甲基系列的N-丁基衍生物中均发现了局部麻醉活性。在剂量水平相当的情况下,这些化合物的活性持续时间比利多卡因长,但比丁卡因短。

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