Mellin C, Vargas H M, Ringdahl B
Department of Pharmacology, School of Medicine, University of California, Los Angeles 90024-1735.
J Med Chem. 1989 Jul;32(7):1590-3. doi: 10.1021/jm00127a031.
Some 3- and 4-bromophenyl and dimethylsulfonium analogues of the muscarinic agent [4-[[N-(3-chlorophenyl)-carbamoyl]oxy]-2-butynyl] trimethylammonium chloride (McN-A-343) (1) were synthesized. The new compounds were assayed for effects on arterial blood pressure in the pithed rat (ganglionic muscarinic activity). The dimethylsulfonium salts (13a-d) appeared to be partial agonists in relation to 1. The 4-bromophenyl-substituted trimethylammonium iodide 10d exceeded 1 in potency by 3-fold. The compounds retained the selectivity for ganglionic muscarinic receptors shown by 1 since they had only weak effects on the guinea pig ileum in vitro.
合成了毒蕈碱剂[4-[[N-(3-氯苯基)-氨基甲酰基]氧基]-2-丁炔基]三甲基氯化铵（McN-A-343）（1）的一些3-和4-溴苯基及二甲基锍类似物。在脊髓切断的大鼠中测定了这些新化合物对动脉血压的影响（神经节毒蕈碱活性）。相对于1，二甲基锍盐（13a-d）似乎是部分激动剂。4-溴苯基取代的三甲基碘化铵10d的效力比1高3倍。这些化合物保留了1所显示的对神经节毒蕈碱受体的选择性，因为它们在体外对豚鼠回肠只有微弱影响。
