Bristow D R, Martin I L
MRC Molecular Neurobiology Unit, MRC Centre, University of Cambridge Medical School, U.K.
Eur J Pharmacol. 1988 Mar 29;148(2):283-8. doi: 10.1016/0014-2999(88)90576-6.
Quantitative receptor autoradiography has been employed to determine the binding distribution of [3H]SR 95531 (2'-(3'-carboxy-2',3'-propyl)-3-amino-6-p-methoxyphenylpyrazinium bromide), a GABAA receptor antagonist, in the rat brain. The location showed good correspondence, in most areas, with the binding of [3H]GABA to GABAA receptors. The major exceptions were binding to cerebellum and hippocampus. We also describe here a non-GABA-associated [3H]SR 95531 binding site which is found at its highest level in the hippocampal CA1 region but also in CA2, CA3, dentate gyrus and cerebral cortex. The results support the localisation of [3H]SR 95531 sites to the GABAA receptor complex.
定量受体放射自显影术已被用于确定GABAA受体拮抗剂[3H]SR 95531(2'-(3'-羧基-2',3'-丙基)-3-氨基-6-对甲氧基苯基吡嗪溴化物)在大鼠脑中的结合分布。在大多数区域,其定位与[3H]GABA与GABAA受体的结合表现出良好的对应关系。主要的例外是与小脑和海马体的结合。我们在此还描述了一个与GABA无关的[3H]SR 95531结合位点,该位点在海马CA1区含量最高,但在CA2、CA3、齿状回和大脑皮层也有发现。这些结果支持了[3H]SR 95531位点定位于GABAA受体复合物。