Nozaki M, Cho T M
J Neurochem. 1985 Aug;45(2):461-4. doi: 10.1111/j.1471-4159.1985.tb04010.x.
Pretreatment of partially purified opiate receptor from rat brains with 5,5'-dithiobis-(2-nitrobenzoic acid) (DTNB) decreased opiate agonist binding more effectively than that of antagonist. This agent, at a concentration that inhibits only 3H-agonist binding, increases the IC50 values of agonists but not those of antagonists. We also observed similar effects of DTNB on opiate binding to the membrane-bound receptor that are in good agreement with the published data. Moreover, there was an excellent correlation between the IC50 values of the two different preparations. However, opiate binding to the partially purified receptor was about a thousandfold more sensitive to DTNB than binding to this membrane-bound receptor. Dithiothreitol, a sulfide bond reducing agent, reversed the effects of DTNB on the opiate binding.
用5,5'-二硫代双(2-硝基苯甲酸)(DTNB)对大鼠脑部分纯化的阿片受体进行预处理，与拮抗剂相比，能更有效地降低阿片激动剂的结合。该试剂在仅抑制3H-激动剂结合的浓度下，增加了激动剂的IC50值，但不增加拮抗剂的IC50值。我们还观察到DTNB对阿片与膜结合受体结合的类似作用，这与已发表的数据高度一致。此外，两种不同制剂的IC50值之间存在极好的相关性。然而，阿片与部分纯化受体的结合对DTNB的敏感性比对该膜结合受体的结合高约一千倍。二硫苏糖醇，一种硫键还原剂，逆转了DTNB对阿片结合的影响。
