CPP，一种新型强效且选择性的N-甲基-D-天冬氨酸（NMDA）拮抗剂。对中枢神经元反应的抑制作用、对脑膜上[3H]D-AP5结合位点的亲和力及抗惊厥活性。

CPP, a new potent and selective NMDA antagonist. Depression of central neuron responses, affinity for [3H]D-AP5 binding sites on brain membranes and anticonvulsant activity.

作者信息

Davies J, Evans R H, Herrling P L, Jones A W, Olverman H J, Pook P, Watkins J C

出版信息

Brain Res. 1986 Sep 10;382(1):169-73. doi: 10.1016/0006-8993(86)90127-7.

Abstract

Properties of a new potent antagonist acting selectively at N-methyl-D-aspartate (NMDA) type excitatory amino acid receptors are described. This compound, 3-((+/-)-2-carboxypiperazin-4-yl)propyl-1-phosphonic acid (CPP) is more potent than all previously reported NMDA antagonists in depressing mammalian spinal neuronal responses (cat and immature rat), in its affinity for [3H]D-AP5 (a radiolabelled NMDA antagonist) binding sites on rat brain membranes, and as an anticonvulsant in mice.

摘要

本文描述了一种新型强效拮抗剂的特性，该拮抗剂可选择性作用于N-甲基-D-天冬氨酸（NMDA）型兴奋性氨基酸受体。这种化合物，即3-（（±）-2-羧基哌嗪-4-基）丙基-1-膦酸（CPP），在抑制哺乳动物脊髓神经元反应（猫和未成熟大鼠）方面、对大鼠脑膜上[3H]D-AP5（一种放射性标记的NMDA拮抗剂）结合位点的亲和力方面以及作为小鼠抗惊厥剂方面，都比所有先前报道的NMDA拮抗剂更有效。