某些与5,6-（亚甲二氧基）茚钙拮抗剂相关的2-取代3-（二甲氨基）-5,6-二甲氧基茚对大鼠回肠的药理学研究。

Pharmacology on rat ileum of certain 2-substituted 3-(dimethylamino)-5,6-dimethoxyindenes related to 5,6-(methylenedioxy)indene calcium antagonists.

作者信息

Witiak D T, Kakodkar S V, Brunst G E, Baldwin J R, Rahwan R G

出版信息

J Med Chem. 1978 Dec;21(12):1313-5. doi: 10.1021/jm00210a028.

Abstract

Whereas the 2-propyl- and 2-butyl-5,6-(methylenedioxy)indene calcium antagonists reversed the spasmogenic action of several agonists including PGF2alpha and acetylcholine at 5 X 10(-5) to 10(-4) M on the rat ileum, the corresponding 5,6-dimethoxy analogues exhibited spasmogenic activity at higher concentration (10(-4)-10(-3) M) and exhibited neither spasmogenic nor spasmolytic activity at lower (10(-6)-10(-5) M) concentration. The results are compared to the methyl and 2-ethyl analogues. At 10(-4) M only the butyl analogue was capable of moderate antagonism of acetylcholine and at 10(-3) M all four analogues were capable of moderately antagonizing the actions of acetylcholine.

摘要

2-丙基和2-丁基-5,6-（亚甲二氧基）茚钙拮抗剂在5×10⁻⁵至10⁻⁴M浓度下可逆转包括PGF2α和乙酰胆碱在内的几种激动剂对大鼠回肠的致痉作用，而相应的5,6-二甲氧基类似物在较高浓度（10⁻⁴ - 10⁻³M）时表现出致痉活性，在较低浓度（10⁻⁶ - 10⁻⁵M）时既不表现出致痉活性也不表现出解痉活性。将这些结果与甲基和2-乙基类似物进行了比较。在10⁻⁴M时，只有丁基类似物能够对乙酰胆碱产生适度拮抗作用，在10⁻³M时，所有四种类似物都能够适度拮抗乙酰胆碱的作用。