フェノチアジン誘導体のジパルミトイルレシチン単分子膜への侵入
1979 年 99 巻 4 号 p. 393-401
詳細
1979 年 99 巻 4 号 p. 393-401
Penetration of a series of phenothiazine derivatives (PTZ) dissolved in phosphate buffer (pH 6.92, ionic strength 0.1) into dipalmitoyl lecithin (DPL) monolayer was studied by the meaeurement of surface pressure (F)-surface area (A) relationships. The surface pressure increase (ΔF) by the penetration of each PTZ into the monolayer under a constant PTZ concentration (10-5M) at a constant molecular area occupied by DPL (75 Å2/molecule) was assumed to be a characteristic parameter on each PTZ, which represents the difference in hydrophile-lipophile balance and affinity to DPL molecule in liquid-expanded state. Relationships between ΔF and some physico-chemical parameters and pharmacological activities, were examined and discussed from the view point of the possibility of employing ΔF as a new physico-chemical parameter which correlates with the pharmacological and clinical potency of psychotropic drugs. The surface pressure increase (ΔF) was found to be correlated with the partition coefficient in n-octanol/water system and also with the surface activity at air-water interface and the protein binding capacity. The correlation between ΔF and some pharmacological activities was also confirmed. Thus, ΔF was suggested to be a valuable parameter, likewise the partition coefficient in oil/water system, which represents quantitatively the difference in pharmacological potency of a series of phenothiazine derivatives.
