Acetylene compounds of potential pharmacological value. XIV. N-(t-aminoalkynyl)-substituted succinimides and maleimides. A class of central anticholinergic agents.
Acetylene compounds of potential pharmacological value. XIV. N-(t-aminoalkynyl)-substituted succinimides and maleimides. A class of central anticholinergic agents.
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具有潜在药理价值的乙炔化合物。
DOI：
10.1021/jm00298a017
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发表时间：
1970
影响因子：
7.3
通讯作者：
J. Giering
中科院分区：
文献类型：
--
作者：
B. Karlén;B. Lindeke;S. Lindgren;K. Svensson;R. Dahlbom;D. Jenden;J. Giering
A series of 34 A7-(<-aminoalkynyl)-substituted succinimides and maleimides has been prepared through the Mannich reaction from an A7-alkynylimide, formaldehyde, and a secondary amine or by ring closure of an N-(t-aminoalkynyl)-substituted succinamic acid. These compounds have been investigatedfor antagonistic activity toward acetylcholine on isolated guinea pig ileal preparations and for mydriaticactivity and blockade of oxo-tremorine in intact mice. Some of the compounds exceed atropine in tremorolyticactivity, and are relatively selective intheir central anticholinergic effects. The latter property tends to be associated with compounds which show evidence of partial agonism in vitro.
