Brown C L, Martin I L
J Neurochem. 1984 Jul;43(1):272-3. doi: 10.1111/j.1471-4159.1984.tb06707.x.
When subjected to ultraviolet light flunitrazepam could be irreversibly attached to brain membrane preparations such that the affinity of the benzodiazepine receptor for certain ligands, such as diazepam, becomes markedly reduced. However, the apparent affinity for diazepam is increased by the addition of gamma-aminobutyric acid and sodium chloride, to the same extent in this membrane preparation as in membranes not so pretreated. This observation suggests that photoaffinity labelling of the benzodiazepine receptor with flunitrazepam modifies the recognition characteristics of the receptor but not its effector mechanism.
当受到紫外线照射时,氟硝西泮可不可逆地附着于脑膜制剂上,使得苯二氮䓬受体对某些配体(如地西泮)的亲和力显著降低。然而,在该脑膜制剂中,加入γ-氨基丁酸和氯化钠后,地西泮的表观亲和力增加,增加程度与未进行如此预处理的膜相同。这一观察结果表明,用氟硝西泮对苯二氮䓬受体进行光亲和标记会改变受体的识别特性,但不会改变其效应机制。