Dobretsov G E, Lyskovtsev V V, Vekshin N L
Farmakol Toksikol. 1979 Mar-Apr;42(2):136-41.
The interaction of thirteen 10-acylaminopropionyl derivatives of phenothiazine with phospholipid membranes was investigated. A correlation between the affinity of these substances to membranes and their antiarrhythmic activity was found. A molecular model of a complex of the substance-membrane is proposed. It shows how the molecular structure of the study substances affects their affinity to phospholipids and thus influences the activity of the former. The affinity chiefly depends on the accordance between the structure and the disposition of the lateral substitute, on the one hand, and the structure of the phospholipid bis-layer, and also of the hydrophobic nature of the 10-acylaminopropionyl group, on the other.
研究了13种吩噻嗪的10-酰氨基丙酰衍生物与磷脂膜的相互作用。发现这些物质对膜的亲和力与其抗心律失常活性之间存在相关性。提出了物质-膜复合物的分子模型。它展示了研究物质的分子结构如何影响其对磷脂的亲和力，进而影响前者的活性。亲和力主要一方面取决于侧链取代基的结构和排列与磷脂双层结构的匹配程度，另一方面还取决于10-酰氨基丙酰基团的疏水性质。
