Rosen G M, Abou-Donia M B, Yeh J Z, Menzel D B
Res Commun Chem Pathol Pharmacol. 1975 Oct;12(2):317-29.
Some spin-labeled acetylcholine analogs, in which the number of methylene groups between the quaternary nitrogen and the ether oxygen ranged between 1-5, were synthesized to study drug interacitons with acetylcholine receptors. None of the compounds tested, with the exception of the one that contained 2 methylene groups (SL-2) had any cholinergic activity. SL-2 was not capable of producing any nicotinic cholinomimetic activity. On the other hand it proved to have a very weak nicotinic cholinolytic activity on the receptors of the frog satorius muscle. This compound exhibited strong antagonism against muscarinic receptors of the isolated frog heart. The muscarinic cholinolytic action of the spin-label ACh analog is discussed in terms of the molecular perturbation theory of drug action.
合成了一些自旋标记的乙酰胆碱类似物，其中季铵氮和醚氧之间的亚甲基数目在1至5之间，以研究药物与乙酰胆碱受体的相互作用。除了含有2个亚甲基的化合物（SL-2）外，所测试的化合物均无胆碱能活性。SL-2不能产生任何烟碱样拟胆碱活性。另一方面，它在青蛙缝匠肌受体上表现出非常弱的烟碱样抗胆碱活性。该化合物对离体青蛙心脏的毒蕈碱受体表现出强烈的拮抗作用。根据药物作用的分子扰动理论讨论了自旋标记的乙酰胆碱类似物的毒蕈碱样抗胆碱作用。
