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philanthotoxin阻断体内由quisqualate、AMPA和kainate诱发的大鼠脑干神经元兴奋,但不阻断NMDA诱发的兴奋。

Philanthotoxin blocks quisqualate-, AMPA- and kainate-, but not NMDA-, induced excitation of rat brainstem neurones in vivo.

作者信息

Jones M G, Anis N A, Lodge D

机构信息

Department of Veterinary Basic Sciences, Royal Veterinary College, London.

出版信息

Br J Pharmacol. 1990 Dec;101(4):968-70. doi: 10.1111/j.1476-5381.1990.tb14189.x.

Abstract
  1. The effect of electrophoretic ejection of philanthotoxin (the polyamine toxin, from the Egyptian digger wasp) was tested on responses of brainstem and spinal neurones in the pentobarbitone-anaesthetized rat to excitatory amino acids. 2. Philanthotoxin caused a dose-dependent reduction of responses to quisqualate, alpha-amino-3-hydroxy-5-phenyl-4-isoxazolepropionate (AMPA) and kainate with little effect on those to N-methyl-D-aspartate (NMDA). 3. The time-course of this antagonist action was slow. In particular the rate of recovery was dependent on frequency of ejection of the agonist. This agonist-dependent recovery suggests that philanthotoxin has a channel blocking mode of action on mammalian central neurones.
摘要
  1. 研究了埃及掘土蜂的多胺毒素 philanthotoxin 的电泳喷射对戊巴比妥麻醉大鼠脑干和脊髓神经元对兴奋性氨基酸反应的影响。2. Philanthotoxin 导致对喹啉酸、α-氨基-3-羟基-5-苯基-4-异恶唑丙酸(AMPA)和海人藻酸的反应呈剂量依赖性降低,而对 N-甲基-D-天冬氨酸(NMDA)的反应影响较小。3. 这种拮抗作用的时间进程较慢。特别是恢复速率取决于激动剂的喷射频率。这种依赖激动剂的恢复表明 philanthotoxin 对哺乳动物中枢神经元具有通道阻断作用模式。

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