Zubenko G S, Cohen B M
Biol Psychiatry. 1985 Apr;20(4):384-96. doi: 10.1016/0006-3223(85)90041-1.
Exposure of normal platelet membranes in vitro to clinically relevant concentrations of phenothiazines has been reported to result in an increase in the structural order of the hydrocarbon region of these membranes (Zubenko and Cohen 1984b,c). In this study, the order parameters (reciprocal of fluidity) of platelet membranes prepared from psychiatric patients receiving phenothiazine antipsychotic drugs were compared to those of an otherwise matched population of psychiatric patients who were not receiving medications that significantly affect this cell membrane property in vitro (Zubenko and Cohen 1984b,c). Membrane order was determined ex vivo by steady-state fluorescence polarization measurements employing 1,6-diphenyl 1,3,5-hexatriene, a fluorescent probe that localizes preferentially in the hydrocarbon region of cell membranes. Phenothiazine administration was associated with a significant increase in platelet membrane order and most likely results from a direct action of these agents on cell membranes. The platelet membrane order parameters of phenothiazine-free patients did not differ significantly from those of a matched group of unmedicated, normal controls. Platelet membrane order was not correlated with daily phenothiazine dose or serum cholesterol concentration. Patient gender did not significantly affect platelet membrane order in any of the groups studied. The potential physiological and clinical significance of phenothiazine-induced increases in cell membrane order is discussed.
据报道,在体外将正常血小板膜暴露于临床相关浓度的吩噻嗪会导致这些膜的烃区域结构有序性增加(祖本科和科恩,1984b,c)。在本研究中,将接受吩噻嗪类抗精神病药物治疗的精神病患者制备的血小板膜的有序参数(流动性的倒数)与未接受在体外会显著影响这种细胞膜特性的药物治疗的其他匹配精神病患者群体的参数进行了比较(祖本科和科恩,1984b,c)。通过使用1,6 - 二苯基 - 1,3,5 - 己三烯进行稳态荧光偏振测量来在体外确定膜的有序性,1,6 - 二苯基 - 1,3,5 - 己三烯是一种优先定位于细胞膜烃区域的荧光探针。服用吩噻嗪与血小板膜有序性显著增加相关,这很可能是这些药物对细胞膜直接作用的结果。未服用吩噻嗪患者的血小板膜有序参数与匹配的未用药正常对照组无显著差异。血小板膜有序性与每日吩噻嗪剂量或血清胆固醇浓度无关。在研究的任何组中,患者性别对血小板膜有序性均无显著影响。本文讨论了吩噻嗪诱导的细胞膜有序性增加的潜在生理和临床意义。