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一种强效的代谢型谷氨酸受体激动剂:一种构象受限的谷氨酸类似物在大鼠脊髓和非洲爪蟾卵母细胞中的电生理作用。

A potent metabotropic glutamate receptor agonist: electrophysiological actions of a conformationally restricted glutamate analogue in the rat spinal cord and Xenopus oocytes.

作者信息

Ishida M, Akagi H, Shimamoto K, Ohfune Y, Shinozaki H

机构信息

Tokyo Metropolitan Institute of Medical Science, Japan.

出版信息

Brain Res. 1990 Dec 24;537(1-2):311-4. doi: 10.1016/0006-8993(90)90375-l.

Abstract

The (2S,3S,4S) isomer of alpha-(carboxycyclopropyl)glycine (L-CCG-I), a conformationally restricted glutamate analogue, caused a marked depolarization of motoneurons in the isolated rat spinal cord, which was almost insensitive to CPP and CNQX. Depolarizing responses to L-CCG-I were markedly decreased by reducing the temperature of the bathing fluid. Similar results were obtained in the case of trans-ACPD, which is a metabotropic glutamate receptor agonist, but the depolarizing action of L-CCG-I was more potent than that of trans-ACPD. In Xenopus oocytes injected with poly(A)+ mRNA extracted from the rat brain, L-CCG-I induced significant oscillatory chloride currents, suggesting that L-CCG-I is a potent agonist for metabotropic-type glutamate receptors.

摘要

α-(羧基环丙基)甘氨酸(L-CCG-I)的(2S,3S,4S)异构体是一种构象受限的谷氨酸类似物,可使离体大鼠脊髓中的运动神经元发生明显去极化,这种去极化对CPP和CNQX几乎不敏感。降低灌流液温度可显著降低对L-CCG-I的去极化反应。代谢型谷氨酸受体激动剂反式-ACPD也得到了类似结果,但L-CCG-I的去极化作用比反式-ACPD更强。在注射了从大鼠脑中提取的聚腺苷酸加尾mRNA的非洲爪蟾卵母细胞中,L-CCG-I诱导出显著的振荡性氯离子电流,这表明L-CCG-I是代谢型谷氨酸受体的有效激动剂。

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