Wong P T, Teo W L
Department of Pharmacology, Faculty of Medicine, National University of Singapore, Republic of Singapore.
Jpn J Pharmacol. 1988 Mar;46(3):261-6. doi: 10.1254/jjp.46.261.
Specific [3H]phenytoin binding in rat cortical membranes is associated with a micromolar affinity site through which diazepam can exert an enhancing effect. In contrast to diazepam, (+)bicuculline, isoguvacine and pentobarbital inhibited phenytoin binding, while GABA and (-)baclofen had no effect. Decreased phenytoin binding and a loss of the diazepam effect were observed in phospholipase A2-treated membranes. Binding in the absence and presence of diazepam demonstrated differential postnatal development. Furthermore, the degree to which binding was enhanced by diazepam varied from one brain region to another. The regional variations of phenytoin binding, both in the presence and absence of diazepam, did not correlate positively with the regional distribution of either the central benzodiazepine receptors or the peripheral type binding sites in the brain.
大鼠皮层膜中特异性的[³H]苯妥英结合与一个微摩尔亲和力位点相关，地西泮可通过该位点发挥增强作用。与地西泮相反，(+)荷包牡丹碱、异谷酰胺和戊巴比妥抑制苯妥英结合，而γ-氨基丁酸（GABA）和(-)巴氯芬则无作用。在磷脂酶A2处理的膜中观察到苯妥英结合减少以及地西泮效应丧失。在有无地西泮情况下的结合表现出不同的出生后发育情况。此外，地西泮增强结合的程度因脑区而异。无论有无地西泮，苯妥英结合的区域差异与脑中中枢苯二氮䓬受体或外周型结合位点的区域分布均无正相关。
