Shevchenko V P, Nagaev I Iu, Vrzheshch P V, Ershov D E, Zaĭtsev S V
Bioorg Khim. 1988 Aug;14(8):1075-85.
A method has been developed that makes it possible to obtain [5,6-3H2]PGE1 with a yield of 35% and a molar radioactivity of 1.7-1.8 TBq/mmol. The binding of [5,6-3H2]PGE1 to native platelets proved to be specific, saturating and reversible. It is characterized by low values (approximately 10(-9) M) of dissociation constants for high-affinity sites, correlates with the inhibition of ADP-induced aggregation of platelets and can be considered as receptor binding. Specific binding of 10 +/- 2 molecules of PGE1 with one platelet was found to cause 50% inhibition of the ADP-induced aggregation.
已开发出一种方法,该方法能够以35%的产率和1.7 - 1.8 TBq/mmol的摩尔放射性获得[5,6 - 3H2]PGE1。事实证明,[5,6 - 3H2]PGE1与天然血小板的结合具有特异性、饱和性和可逆性。其特点是高亲和力位点的解离常数较低(约10^(-9) M),与ADP诱导的血小板聚集抑制相关,可被视为受体结合。发现每一个血小板与10 ± 2个PGE1分子的特异性结合会导致ADP诱导的聚集受到50%的抑制。