Spero L
Can J Physiol Pharmacol. 1978 Oct;56(5):873-6. doi: 10.1139/y78-136.
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.
在经二苯那明预处理的兔胃平滑肌上测试了阿托品与完全激动剂卡巴胆碱之间的竞争性。即使在经二苯那明进行广泛的不可逆阻断后,阿托品对卡巴胆碱反应的阻断仍具有竞争性,且阿托品的亲和力常数未改变。这与阿托品阻断毛果芸香碱或庚基三甲基铵等部分激动剂的收缩作用时的非竞争性作用不同。因此,结果表明,仅仅通过减少可用胆碱能受体的数量,不可能将完全激动剂转化为部分激动剂。本研究比较了在不可逆阻断条件下,阿托品对完全激动剂卡巴胆碱作用的竞争性效应,与阿托品对毛果芸香碱或庚基三甲基铵等部分激动剂的竞争性效应。