Kiskin N I, Kryshtal' O A, Tsyndrenko A Ia, Volkova T M, Grishin E V
Neirofiziologiia. 1989;21(6):748-56.
Several homologous low-molecular weight compounds were purified from venom of spider Argiope lobata. They selectively blocked ionic currents elicited by glutamate and its agonist kainate in the membrane of isolated hippocampal neurons of rat. Three groups of these compounds--argiopine, argiopinines and pseudoargiopinines, blocked glutamate- and kainate-activated ionic currents in a voltage-dependent manner, acting preferentially on agonist-activated ionic channels. These compounds did not change the Kd values for both agonists. The blocking action was partially reversible for argiopine and poorly reversible for other compounds. Rate constants for the interaction of toxins with membrane receptors were estimated from the dependences of two-component kinetics of the blocking action and its recovery on toxin concentrations. Argiopine, argiopinines and pseudoargiopinines may be useful tools for further electrophysiological and biochemical investigation of the mammalian CNS glutamate receptors.
从蜘蛛棒络新妇的毒液中纯化出了几种同源的低分子量化合物。它们选择性地阻断了谷氨酸及其激动剂海人酸在大鼠离体海马神经元膜上引发的离子电流。这些化合物的三组——棒络新妇碱、棒络新妇次碱和假棒络新妇碱，以电压依赖性方式阻断谷氨酸和海人酸激活的离子电流，优先作用于激动剂激活的离子通道。这些化合物并未改变两种激动剂的解离常数。棒络新妇碱的阻断作用部分可逆，而其他化合物的阻断作用则难以逆转。根据阻断作用及其恢复的双组分动力学对毒素浓度的依赖性，估算了毒素与膜受体相互作用的速率常数。棒络新妇碱、棒络新妇次碱和假棒络新妇碱可能是进一步对哺乳动物中枢神经系统谷氨酸受体进行电生理和生化研究的有用工具。
