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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.

DOI:10.1016/0006-8993(90)90375-l
PMID:1964837
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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A potent metabotropic glutamate receptor agonist: electrophysiological actions of a conformationally restricted glutamate analogue in the rat spinal cord and Xenopus oocytes.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。
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引用本文的文献

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Synaptic control of motoneuronal excitability.运动神经元兴奋性的突触控制
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2
Pharmacological characterization of metabotropic glutamate receptors potentiating NMDA responses in mouse cortical wedge preparations.代谢型谷氨酸受体增强小鼠皮质楔形标本中NMDA反应的药理学特征
Br J Pharmacol. 1996 Jul;118(6):1530-6. doi: 10.1111/j.1476-5381.1996.tb15570.x.
3
Structure-activity relationships of new agonists and antagonists of different metabotropic glutamate receptor subtypes.
不同代谢型谷氨酸受体亚型新型激动剂和拮抗剂的构效关系
Br J Pharmacol. 1996 Apr;117(7):1493-503. doi: 10.1111/j.1476-5381.1996.tb15312.x.
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A novel metabotropic glutamate receptor agonist: marked depression of monosynaptic excitation in the newborn rat isolated spinal cord.一种新型代谢型谷氨酸受体激动剂:新生大鼠离体脊髓单突触兴奋的显著抑制
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Pharmacological characterization of the metabotropic glutamate receptor inhibiting D-[3H]-aspartate output in rat striatum.代谢型谷氨酸受体抑制大鼠纹状体中D-[3H]-天冬氨酸输出的药理学特性
Br J Pharmacol. 1993 Dec;110(4):1407-12. doi: 10.1111/j.1476-5381.1993.tb13977.x.
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Agonist analysis of 2-(carboxycyclopropyl)glycine isomers for cloned metabotropic glutamate receptor subtypes expressed in Chinese hamster ovary cells.对在中华仓鼠卵巢细胞中表达的克隆代谢型谷氨酸受体亚型的2-(羧基环丙基)甘氨酸异构体进行激动剂分析。
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