Sowell J W, Block A J, Derrick M E, Freeman J J, Kosh J W, Mattson R J, Mubarak P F, Tenthorey P A
J Pharm Sci. 1981 Feb;70(2):135-40. doi: 10.1002/jps.2600700206.
The synthesis, local anesthetic and antiarrhythmic properties, and CNS toxicity of 19 2-(2-alkylaminoalkylamido)pyrroles are described. Most of the compounds exhibited local anesthetic activity by the guinea pig wheal test, and four showed activity comparable to or greater than that of lidocaine. Most compounds also exhibited antiarrhythmic activity; five compounds had activity comparable to that of lidocaine, and one was more potent. All compounds exhibiting antiarrhythmic activity also were toxic to the central nervous system.
描述了19种2-(2-烷基氨基烷基酰胺基)吡咯的合成、局部麻醉和抗心律失常特性以及中枢神经系统毒性。大多数化合物通过豚鼠风团试验表现出局部麻醉活性，其中四种化合物的活性与利多卡因相当或更强。大多数化合物还表现出抗心律失常活性；五种化合物的活性与利多卡因相当，一种更有效。所有表现出抗心律失常活性的化合物对中枢神经系统也有毒性。
