Keenan T H, Freeman J J, Sowell J W, Kosh J W
Pharmacology. 1979;19(1):36-43. doi: 10.1159/000137280.
Three analogs of lidocaine (benzyl carbamyl, benzyl nitrile and methyl nitrile) were synthesized and examined for cardiovascular and central activity. The benzyl carbamyl analog was more potent than lidocaine in lowering blood pressure but possessed only slight local anesthetic, antiarrhythmic and CNS-depressant activity. At 40 mg/kg the benzyl nitrile derivative was superior to lidocaine in protecting against chloroform-induced arrhythmias. The methyl nitrile analog was less active than the benzyl nitrile analog in most parameters examined. The benzyl nitrile derivative and lidocaine had similar potencies on blood pressure depression, local anesthetic activity and ability to protect against calcium chloride-induced arrhythmias. Unlike the benzyl carbamyl derivative both lidocaine and the benzyl nitrile compounds appear to depress the cardiovascular system via a common mechanism.
合成了利多卡因的三种类似物（苄基甲酰基、苄基腈和甲基腈），并对其心血管和中枢活性进行了检测。苄基甲酰基类似物在降低血压方面比利多卡因更有效，但仅具有轻微的局部麻醉、抗心律失常和中枢神经系统抑制活性。在40mg/kg时，苄基腈衍生物在预防氯仿诱导的心律失常方面优于利多卡因。在大多数检测参数中，甲基腈类似物的活性低于苄基腈类似物。苄基腈衍生物和利多卡因在降低血压、局部麻醉活性以及预防氯化钙诱导的心律失常能力方面具有相似的效力。与苄基甲酰基衍生物不同，利多卡因和苄基腈化合物似乎通过共同机制抑制心血管系统。
