Bae S J, Kitamura S, Herbette L G, Sturtevant J M
Department of Chemistry, Yale University, New Haven, CT 06511.
Chem Phys Lipids. 1989 Jul;51(1):1-7. doi: 10.1016/0009-3084(89)90059-5.
The effects of four calcium channel blocking drugs, diltiazem, verapamil, nimodipine and nisoldipine, on the main phase transition of dimyristoylphosphatidylcholine have been studied by high resolution differential scanning calorimetry. In all cases, the phase transition temperature is lowered, though much more effectively by nimodipine and nisoldipine than by the other two drugs. Nimodipine and nisoldipine markedly reduce the enthalpy of transition while diltiazem and verapamil have no significant effect on the enthalpy within the drug concentration range studied. Analysis of the data in terms of ideal solution theory is presented. X-ray and neutron scattering studies indicate that nimodipine and verapamil differ significantly with respect to their location within a lipid bilayer, and this difference suggests a partial rationalization of the experimental results presented here.
通过高分辨率差示扫描量热法研究了四种钙通道阻滞剂，即地尔硫䓬、维拉帕米、尼莫地平和尼索地平对二肉豆蔻酰磷脂酰胆碱主相变的影响。在所有情况下，相变温度均降低，不过尼莫地平和尼索地平比其他两种药物的作用更显著。尼莫地平和尼索地平显著降低了转变焓，而在地尔硫䓬和维拉帕米的研究药物浓度范围内，它们对焓没有显著影响。本文根据理想溶液理论对数据进行了分析。X射线和中子散射研究表明，尼莫地平和维拉帕米在脂质双层中的位置有显著差异，这种差异为此处呈现的实验结果提供了部分合理的解释。
