大鼠脊髓中静脉注射AMPA拮抗剂NBQX和GYKI 53655的比较。
A comparison of intravenous NBQX and GYKI 53655 as AMPA antagonists in the rat spinal cord.
作者信息
Chizh B A, Cumberbatch M J, Headley P M
机构信息
Department of Physiology, School of Medical Sciences, University of Bristol.
出版信息
Br J Pharmacol. 1994 Jul;112(3):843-6. doi: 10.1111/j.1476-5381.1994.tb13156.x.
Abstract
- The effects of intravenous administration of two alpha-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonists were studied on responses of single neurones to iontophoretically applied excitatory amino acids. The tests were performed on spinal neurones in alpha-chloralose anaesthetized, spinalized rats. 2. Both the quinoxaline, NBQX (2-16 mg kg-1) and the 2,3-benzodiazepine, GYKI 53655 (2-8 mg kg-1) dose-dependently decreased responses to AMPA. 3. Both compounds were short acting, with half-recovery times of 15 min for NBQX and 7 min for GYKI 53655. 4. The selectivity for responses to AMPA over those to N-methyl-D-aspartate (NMDA) was significantly poorer for systemic NBQX than for either systemic GYKI 53655 or iontophoretic NBQX, suggesting that systemic NBQX may be converted to a less selective metabolite. 5. GYKI 53655 is therefore likely to be a more valuable tool than NBQX for the study of AMPA receptor-mediated processes in vivo.
摘要
- 研究了静脉注射两种α-氨基-3-羟基-5-甲基异恶唑-4-丙酸（AMPA）拮抗剂对单个神经元对离子导入兴奋性氨基酸反应的影响。实验在α-氯醛糖麻醉、脊髓横断的大鼠的脊髓神经元上进行。2. 喹喔啉类的NBQX（2 - 16毫克/千克）和2,3-苯并二氮杂䓬类的GYKI 53655（2 - 8毫克/千克）均剂量依赖性地降低了对AMPA的反应。3. 两种化合物作用时间均较短，NBQX的半恢复时间为15分钟，GYKI 53655为7分钟。4. 全身应用NBQX时，对AMPA反应的选择性比对N-甲基-D-天冬氨酸（NMDA）反应的选择性明显低于全身应用GYKI 53655或离子导入NBQX的情况，这表明全身应用的NBQX可能转化为选择性较低的代谢产物。5. 因此，对于体内AMPA受体介导过程的研究，GYKI 53655可能是比NBQX更有价值的工具。
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本文引用的文献
1
A benzodiazepine recognition site associated with the non-NMDA glutamate receptor.
Neuron. 1993 Jan;10(1):61-7. doi: 10.1016/0896-6273(93)90242-j.
2
An analysis of synaptic transmission to motoneurones in the cat spinal cord using a new selective receptor blocker.
Acta Physiol Scand. 1993 Jun;148(2):97-100. doi: 10.1111/j.1748-1716.1993.tb09537.x.
3
GYKI 52466, a 2,3-benzodiazepine, is a highly selective, noncompetitive antagonist of AMPA/kainate receptor responses.
Neuron. 1993 Jan;10(1):51-9. doi: 10.1016/0896-6273(93)90241-i.
4
Effect of glutamate receptor antagonists on N-methyl-D-aspartate- and (S)-alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid-induced convulsant effects in mice and rats.
Eur J Pharmacol. 1993 Oct 5;242(3):213-20. doi: 10.1016/0014-2999(93)90244-c.
5
Therapeutic potential of excitatory amino acid antagonists: channel blockers and 2,3-benzodiazepines.
Trends Pharmacol Sci. 1993 Sep;14(9):325-31. doi: 10.1016/0165-6147(93)90005-5.
6
Quinoxalinediones: potent competitive non-NMDA glutamate receptor antagonists.
Science. 1988 Aug 5;241(4866):701-3. doi: 10.1126/science.2899909.
7
The role of N-methylaspartate receptors in mediating responses of rat and cat spinal neurones to defined sensory stimuli.
J Physiol. 1987 Apr;385:169-88. doi: 10.1113/jphysiol.1987.sp016490.
8
2,3-Dihydroxy-6-nitro-7-sulfamoyl-benzo(F)quinoxaline: a neuroprotectant for cerebral ischemia.
Science. 1990 Feb 2;247(4942):571-4. doi: 10.1126/science.2154034.
9
Excitatory amino acids: new tools for old stories or pharmacological subtypes of glutamate receptors: electrophysiological studies.
Can J Physiol Pharmacol. 1991 Jul;69(7):1123-8. doi: 10.1139/y91-164.
10
Pharmacological characterization of non-NMDA subtypes of glutamate receptor in the neonatal rat hemisected spinal cord in vitro.
Br J Pharmacol. 1992 Jun;106(2):367-72. doi: 10.1111/j.1476-5381.1992.tb14342.x.
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