(R)-HA-966对[3H]CPP与NMDA受体复合物结合的立体选择性增强作用。
Stereoselective enhancement by (R)-HA-966 of the binding of [3H]CPP to the NMDA receptor complex.
作者信息
Pullan L M, Powel R J, Stumpo R J, Britt M, Klika A B, Meiners B A, Salama A I
机构信息
ICI Pharmaceuticals Group, ICI Americas, Inc., Wilmington, DE 19897.
出版信息
Eur J Pharmacol. 1990 Sep 18;189(2-3):237-40. doi: 10.1016/0922-4106(90)90029-w.
The enantiomers of the strychnine-insensitive glycine antagonist, HA-966 (1-hydroxy-3-amino-pyrrolidone-2), stereoselectively enhance binding of the N-methyl-D-aspartate (NMDA) competitive antagonist, [3H]CPP (3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid) to rat brain synaptosomal membranes. The enhancement by the more potent (R)-HA-966 is competitively inhibited by the glycine antagonist 7-chlorokynurenic acid and noncompetitively by the polyamine spermine. Thus, (R)-HA-966, apparently at the glycine site, enhances the binding of antagonist to the NMDA receptor, possibly through a mechanism partially in common with that of spermine.
士的宁不敏感型甘氨酸拮抗剂HA-966（1-羟基-3-氨基-吡咯烷酮-2）的对映体，能立体选择性地增强N-甲基-D-天冬氨酸（NMDA）竞争性拮抗剂[3H]CPP（3-(2-羧基哌嗪-4-基)丙基-1-膦酸）与大鼠脑突触体膜的结合。更强效的(R)-HA-966所产生的增强作用，受到甘氨酸拮抗剂7-氯犬尿氨酸的竞争性抑制，并受到多胺精胺的非竞争性抑制。因此，(R)-HA-966显然是在甘氨酸位点，可能通过一种部分与精胺相同的机制，增强拮抗剂与NMDA受体的结合。
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