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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Chizh B A, Cumberbatch M J, Headley P M

Department of Physiology, School of Medical Sciences, University of Bristol.

Br J Pharmacol. 1994 Jul;112(3):843-6. doi: 10.1111/j.1476-5381.1994.tb13156.x.

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.

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。

Chizh B A, Cumberbatch M J, Headley P M

Department of Physiology, School of Medical Sciences, University of Bristol.

Br J Pharmacol. 1994 Jul;112(3):843-6. doi: 10.1111/j.1476-5381.1994.tb13156.x.

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.

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。