Abood L G, Takeda F
Eur J Pharmacol. 1976 Sep;39(1):71-7. doi: 10.1016/0014-2999(76)90114-x.
An effort was made to elucidate the possible involvement of phosphatidyl serine in the opiate receptor by examining stereospecific 3H-dihydromorphine binding to neural membrane preparations in the presence of exogenous phosphatidyl serine. The addition of phosphatidyl serine to suspensions of either synaptic membranes or a microsomal fraction significantly enhanced both high and lower affinity binding, the Kd's being 1.0 X 10(-9) and 5.7 X 10(-9) M without lipid and 5.0 X 10(-10) and 3.8 X 10(-9) M with added phosphatidyl serine. Phosphatidyl ethanolamine and lysophosphatidyl ethanolamine had an inhibitory effect on opiate binding. Sulfatides had a slight enhancing effect, while other acidic lipids and lecithin were without any effect. With the use of 3H-dansyl phosphatidyl serine it was established that sufficient exogenous lipid was associated with the membrane to account for the enhancement of opiate binding. The results were discussed from the standpoint of the modification of membrane lipids and their possible significance for the binding of opiates and other ligands. It is suggested that phosphatidyl serine may be an important component of the opiate pharmacophore.
通过检测在外源磷脂酰丝氨酸存在的情况下立体特异性3H - 二氢吗啡与神经膜制剂的结合，来努力阐明磷脂酰丝氨酸在阿片受体中的可能作用。向突触膜或微粒体部分的悬浮液中添加磷脂酰丝氨酸，显著增强了高亲和力和低亲和力结合，无脂质时Kd值分别为1.0×10⁻⁹和5.7×10⁻⁹M，添加磷脂酰丝氨酸后Kd值分别为5.0×10⁻¹⁰和3.8×10⁻⁹M。磷脂酰乙醇胺和溶血磷脂酰乙醇胺对阿片结合有抑制作用。硫苷脂有轻微增强作用，而其他酸性脂质和卵磷脂则无任何作用。使用3H - 丹磺酰磷脂酰丝氨酸确定，有足够的外源脂质与膜结合，以解释阿片结合的增强。从膜脂质修饰及其对阿片和其他配体结合的可能意义的角度讨论了结果。提示磷脂酰丝氨酸可能是阿片药效基团的重要组成部分。
