Nesterov V P, Matveev V V, Demina I N, Logosha S A
Biofizika. 1996 Jan-Feb;41(1):110-5.
Verapamil, general and local anesthetics influences on ionic contents of frog sartorius and cardiac muscles in respect with these drugs hydrophobicity were studied to clarify the role of verapamil hydrophobic interactions in its physiological activity. It was found that concentration thresholds of the agents toxicities were linearly linked with their hydrophobicity (in logarithmic scale). This relationship provides support for our conclusion that verapamil, general and some local anesthetics are the members of a single drug family. It is a reason to believe that a hydrophobic mechanism of general anesthetic action on cellular structure is the same as a mechanism of verapamil activity in muscles. It is possible that verapamil is accepted as medical drug exactly due to optimum combination of high verapamil hydrophobicity with its structural complementarity to receptor site responsible for use-dependent channel blocking.
研究了维拉帕米、全身麻醉药和局部麻醉药对青蛙缝匠肌和心肌离子含量的影响，涉及这些药物的疏水性，以阐明维拉帕米疏水相互作用在其生理活性中的作用。发现这些药物毒性的浓度阈值与其疏水性呈线性相关（对数尺度）。这种关系支持了我们的结论，即维拉帕米、全身麻醉药和一些局部麻醉药属于同一类药物家族。有理由相信全身麻醉药对细胞结构的疏水作用机制与维拉帕米在肌肉中的活性机制相同。维拉帕米被用作药物，可能正是由于其高疏水性与其对负责使用依赖性通道阻断的受体位点的结构互补性的最佳结合。
