一种由红藻氨酸和L-谷氨酸衍生而来的二肽：一种具有抗惊厥特性的氨基酸诱导神经兴奋的选择性拮抗剂。

A dipeptide derived from kainic and L-glutamic acids: a selective antagonist of amino acid induced neuroexcitation with anticonvulsant properties.

作者信息

Goldberg O, Teichberg V I

出版信息

J Med Chem. 1985 Dec;28(12):1957-8. doi: 10.1021/jm00150a034.

Abstract

The dipeptide N-[[[2'S-(2' alpha, 3' beta, 4' beta)]-2'-carboxy-4'-(1"-methylethenyl)-3'-pyrrolidinyl)acetyl]-L- glutamic acid (6) has been synthesized by a route that involves the selective protection of the alpha-carboxyl function of kainic acid. This dipeptide inhibits the stimulation of Na+ fluxes induced in brain slices by the neuroexcitant N-methyl-D-aspartic acid. Administered intracerebroventricularly, it is also effective in protecting mice from picrotoxin-induced convulsions with an ED50 of 0.17 mumol.

摘要

二肽N-[[[2'S-(2'α, 3'β, 4'β)]-2'-羧基-4'-(1"-甲基乙烯基)-3'-吡咯烷基]乙酰基]-L-谷氨酸(6)已通过一种涉及对海藻酸α-羧基功能进行选择性保护的路线合成。该二肽可抑制神经兴奋性物质N-甲基-D-天冬氨酸在脑切片中诱导的Na+通量的刺激。经脑室内给药时，它对保护小鼠免受印防己毒素诱导的惊厥也有效，半数有效剂量(ED50)为0.17 μmol。