Atropine blockade of cholinergic drugs on rabbit stomach muscle.
The competition between atropine and a full agonist, carbachol, was tested on dibenamine-pretreated smooth muscle of rabbit stomach. Even after extensive irreversible blockade by dibenamine, atropine blockade of the response to carbachol was still competitive and the atropine affinity constant was unchanged. This differed from the noncompetitive action of atropine in blocking the contractile effects of partial agonists such as pilocarpine or heptyl trimethylammonium. The results thus indicate that it is not possible to convert a full agonist into a partial agonist merely by reducing the number of available cholinergic receptors. The present study compares the competitive effect of atropine on the actions of the full agonist carbachol, under conditions of irreversible blockade, with the competitive effect of atropine on partial agonists such as pilocarpine or heptyl trimethylammonium.
D000818:Animals; D001285:Atropine / Q000494:pharmacology*; D002217:Carbachol / Q000037:antagonists & inhibitors; D003983:Dibenzylchlorethamine / Q000494:pharmacology; D066298:In Vitro Techniques; D009119:Muscle Contraction / Q000187:drug effects*; D009130:Muscle, Smooth / Q000187:drug effects*; D010276:Parasympatholytics; D010862:Pilocarpine / Q000037:antagonists & inhibitors; D000644:Quaternary Ammonium Compounds / Q000037:antagonists & inhibitors; D011817:Rabbits; D013270:Stomach / Q000187:drug effects
D010276:Parasympatholytics; D000644:Quaternary Ammonium Compounds; D010862:Pilocarpine; D003983:Dibenzylchlorethamine; D001285:Atropine; D002217:Carbachol