Pharmacology on rat ileum of certain 2-substituted 3-(dimethylamino)-5,6-dimethoxyindenes related to 5,6-(methylenedioxy)indene calcium antagonists.
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.
D000109:Acetylcholine / Q000037:antagonists & inhibitors; D000818:Animals; D005260:Female; D007082:Ileum / Q000187:drug effects; D066298:In Vitro Techniques; D007192:Indenes / Q000138:chemical synthesis / Q000494:pharmacology*; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D011460:Prostaglandins F / Q000037:antagonists & inhibitors; D051381:Rats; D013329:Structure-Activity Relationship
D007192:Indenes; D011460:Prostaglandins F; D000109:Acetylcholine