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NMDA拮抗剂CPP和CGS 19755对中枢苯二氮䓬受体缺乏亲和力。

The NMDA antagonists, CPP and CGS 19755, lack affinity for central benzodiazepine receptors.

作者信息

Williams M, Loo P S, Sills M A

机构信息

Research Department, Ciba-Geigy Corporation, Summit, NJ 07901.

出版信息

Eur J Pharmacol. 1988 Oct 11;155(1-2):185-7. doi: 10.1016/0014-2999(88)90421-9.

Abstract

CPP (3-(2-carboxypiperazin-4-yl-propyl-1-phosphonic acid), a rigid analog of AP7 (2-amino-7-phosphonoheptanoate), previously shown to be a selective antagonist of the NMDA (N-methyl-D-aspartate) receptor (IC50 = 209 nM) has been reported to be exceptionally active (IC50 = 430 pM) at benzodiazepine binding sites. Re-examination of CPP, and the rigid AP5 analog, CGS 19755 (cis-4-phosphonomethyl-2-piperidine carboxylic acid; 0.001-10,000 nM), showed that, as previously reported, neither compound affected the binding of [3H]flunitrazepam. These compounds are thus selective NMDA receptor antagonists.

摘要

CPP(3 -(2 - 羧基哌嗪 - 4 - 基)丙基 - 1 - 膦酸),AP7(2 - 氨基 - 7 - 膦酰庚酸)的刚性类似物,先前已证明是NMDA(N - 甲基 - D - 天冬氨酸)受体的选择性拮抗剂(IC50 = 209 nM),据报道在苯二氮䓬结合位点具有异常活性(IC50 = 430 pM)。对CPP以及刚性AP5类似物CGS 19755(顺式 - 4 - 膦酰甲基 - 2 - 哌啶羧酸;0.001 - 10,000 nM)的重新检测表明,如先前报道的那样,这两种化合物均不影响[3H]氟硝西泮的结合。因此,这些化合物是选择性NMDA受体拮抗剂。

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