论文部分内容阅读
作者曾报导,(Ⅰ)具有较好的浸润、传导及表面局部麻醉作用,并且毒性较低,局部耐受性也佳。作者通过A的变换以影响分子的亲水性能,而在苯环上引入取代基或用烷芳基取代苯基以改变分子的亲脂性能,希望获得具最适局部麻醉性能的药物。共合成了57个化合物,经药理试验表明Ⅱ_a(R=2-CH_3,n=0,A=-CH_2-CH_2-)的局部耐受性与利多卡因及普鲁卡因相似,而其毒性及局部麻醉作用(浸润、传导、表面)均较利多卡因、普鲁卡因为佳。现已进入深入的药理、毒性及临床研究。
The authors have reported, (Ⅰ) has good infiltration, conduction and surface anesthesia, and less toxic, local tolerance is also good. The author through the transformation of A to affect the hydrophilic properties of molecules, and the introduction of benzene ring substituents or aryl-substituted phenyl to change the lipophilic properties of the molecule, hoping to obtain the most appropriate local anesthetic properties of the drug. A total of 57 compounds were synthesized and pharmacologically indicated that local toxicity of Ⅱ_a (R = 2-CH_3, n = 0, A = -CH_2-CH_2-) was similar to that of lidocaine and procaine, And local anesthesia (infiltration, conduction, surface) than lidocaine, proca better. Has now entered the depth of pharmacology, toxicity and clinical research.