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精胺对NMDA受体的激活需要谷氨酸,但不需要甘氨酸。

NMDA receptor activation by spermine requires glutamate but not glycine.

作者信息

Marvizón J C, Baudry M

机构信息

Neurobiology Program, University of Southern California, Los Angeles 90089-2520.

出版信息

Eur J Pharmacol. 1993 Jan 4;244(1):103-4. doi: 10.1016/0922-4106(93)90065-h.

DOI:10.1016/0922-4106(93)90065-h
PMID:8093599
Abstract

Stimulation by spermine of [3H]MK-801 binding to N-methyl-D-aspartate (NMDA) receptors was additive with the effect of glutamate and glycine, but was completely abolished by the glutamate antagonist 3-(carboxypiperazin-4-yl)propyl-1-phosphonate (CPP, 10 microM) or the glycine antagonist 7-chlorokynurenate (10 microM). Blockade by 7-chlorokynurenate could be overcome in the presence of glutamate, whereas blockade by CPP was unaffected by glycine. Therefore, NMDA receptors can be activated by glutamate and spermine but not by glycine and spermine.

摘要

精胺对[3H]MK-801与N-甲基-D-天冬氨酸(NMDA)受体结合的刺激作用与谷氨酸和甘氨酸的作用呈相加性,但完全被谷氨酸拮抗剂3-(羧基哌嗪-4-基)丙基-1-膦酸(CPP,10微摩尔)或甘氨酸拮抗剂7-氯犬尿氨酸(10微摩尔)所消除。在存在谷氨酸的情况下,7-氯犬尿氨酸的阻断作用可被克服,而CPP的阻断作用不受甘氨酸影响。因此,NMDA受体可被谷氨酸和精胺激活,但不能被甘氨酸和精胺激活。

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1
NMDA receptor activation by spermine requires glutamate but not glycine.精胺对NMDA受体的激活需要谷氨酸,但不需要甘氨酸。
Eur J Pharmacol. 1993 Jan 4;244(1):103-4. doi: 10.1016/0922-4106(93)90065-h.
2
Inhibition of [3H]-(+)-MK 801 binding to rat brain sections by CPP and 7-chlorokynurenic acid: an autoradiographic analysis.
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Allosteric interactions and modulator requirement for NMDA receptor function.N-甲基-D-天冬氨酸受体功能的变构相互作用及调节剂需求
Eur J Pharmacol. 1994 Oct 14;269(2):165-75. doi: 10.1016/0922-4106(94)90083-3.
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Regionally distinct N-methyl-D-aspartate receptors distinguished by quantitative autoradiography of [3H]MK-801 binding in rat brain.通过对大鼠脑内[3H]MK-801结合进行定量放射自显影区分区域不同的N-甲基-D-天冬氨酸受体。
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An antagonist/partial agonist at the polyamine recognition site of the N-methyl-D-aspartate receptor that alters the properties of the glutamate recognition site.一种作用于N-甲基-D-天冬氨酸受体多胺识别位点的拮抗剂/部分激动剂,可改变谷氨酸识别位点的特性。
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Polyamine effects upon N-methyl-D-aspartate receptor functioning: differential alteration by glutamate and glycine site antagonists.多胺对N-甲基-D-天冬氨酸受体功能的影响:谷氨酸和甘氨酸位点拮抗剂的差异改变
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Na+, K+ and Ca2+ antagonize the glutamate- and glycine-induced decrease of [3H]MK-801 binding observed in the presence of Mg2+ at low pH.在低pH值且存在镁离子的情况下,钠离子、钾离子和钙离子可拮抗由谷氨酸和甘氨酸诱导的[3H]MK-801结合的减少。
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Glutamate and glycine co-activate while polyamines merely modulate the NMDA receptor complex.谷氨酸和甘氨酸共同激活,而多胺仅调节NMDA受体复合物。
Prog Neuropsychopharmacol Biol Psychiatry. 1991;15(2):183-90. doi: 10.1016/0278-5846(91)90079-g.

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