Jarvis M F, Murphy D E, Williams M
Pharmaceuticals Division, Ciba-Geigy Corporation, Summit, NJ 07901.
Eur J Pharmacol. 1987 Sep 2;141(1):149-52. doi: 10.1016/0014-2999(87)90423-7.
The regional distribution of N-methyl-D-aspartate (NMDA) receptors in rat brain using the selective NMDA receptor ligand [3H]3-[+/-)-2-carboxypiperazin-4-yl)propyl-1-phosphonic acid (CPP) has been quantitated by in vitro autoradiography. [3H]CCP binding was highest in the CA1 region of the hippocampus. Relatively high levels of binding were also observed in the cerebral cortex, while moderate binding was obtained in the thalamus, striatum and granule cell layer of the cerebellum. Concurrent studies examining the phencyclidine receptor ligand [3H]1-[1-(2-thienyl)cyclohexyl]-piperidine (TCP), revealed a similar pattern of binding that correlated well with the localization of [3H]CPP-labeled NMDA receptors (r = 0.88, P less than 0.01).
利用选择性N-甲基-D-天冬氨酸(NMDA)受体配体[3H]3-[(±)-2-羧基哌嗪-4-基]丙基-1-膦酸(CPP),通过体外放射自显影法对大鼠脑中NMDA受体的区域分布进行了定量分析。[3H]CCP结合在海马体的CA1区域最高。在大脑皮层也观察到相对较高水平的结合,而在丘脑、纹状体和小脑颗粒细胞层则获得中等水平的结合。同时研究苯环己哌啶受体配体[3H]1-[1-(2-噻吩基)环己基]-哌啶(TCP),发现了相似的结合模式,与[3H]CPP标记的NMDA受体的定位密切相关(r = 0.88,P < 0.01)。