Urenjak J, Tegtmeier F, Beile A, Khan S, Peters T
Department of Experimental Medicine, Janssen Research Foundation, Neuss, FRG.
Pharmacology. 1991;43(1):26-35. doi: 10.1159/000138824.
Inhibition of the voltage-dependent Na channel by tetrodotoxin (5 mumol/l) decreased by about 86% the stimulation of the respiration of rat brain synaptosomes induced by veratridine (10 mumol/l). A similar effect was achieved by blocking Na(+)-K(+)-ATPase with ouabain (1 mmol/l). Pharmacological manipulations of Ca homeostasis suggested that the veratridine-induced stimulation of respiration did not depend upon Ca entry. These data suggest that the veratridine-induced stimulation of synaptosomal respiration may result primarily from an increase in intracellular Na+. They provide the basis for an indirect method, which only requires recording of synaptosomal respiration, to test drugs for their possible interaction with excessive Na influxes.
河豚毒素(5微摩尔/升)对电压依赖性钠通道的抑制作用使藜芦定(10微摩尔/升)诱导的大鼠脑突触体呼吸刺激降低了约86%。用哇巴因(1毫摩尔/升)阻断钠钾ATP酶也产生了类似的效果。对钙稳态的药理学操作表明,藜芦定诱导的呼吸刺激并不依赖于钙的内流。这些数据表明,藜芦定诱导的突触体呼吸刺激可能主要源于细胞内钠离子的增加。它们为一种间接方法提供了基础,该方法仅需记录突触体呼吸,即可测试药物与过量钠内流可能的相互作用。