Langer S Z, Adler-Graschinsky E, Almeida A P, Diniz C R
Naunyn Schmiedebergs Arch Pharmacol. 1975;287(3):243-59. doi: 10.1007/BF00501471.
The effects of a purified fraction of the venom of the Brazilian scorpion, Tityus serrulatus, were studied in isolated guinea-pig atria previously labelled with 3H-noradrenaline. Exposure to 0.3 and 1.0 mug/ml of the scorpion toxin resulted in a long lasting positive chronotropic effect which was concentration-dependent. The increase in atrial rate coincided with an enhancement in spontaneous outflow of radioactivity. The increase in outflow of radioactive products elicited by exposure to 1.0 mug/ml of the scorpion toxin was approximately 3-fold. 3H-noradrenaline accounted for 60% of the total increase in outflow of radioactivity elicited by the scorpion toxin and the 3H-deaminated glycol (3,4-dihydroxyphenyl-glycol) represented the main metabolite formed, accounting for approximately 35% of the total release. 20 min after exposure to 1.0 mug/ml of the scorpion toxin the overflow of the labelled transmitter elicited by accelerans nerve stimulation (4 Hz, during 60 sec. supramaximal voltage) was increased 8-fold. This effect of the scorpion toxin appears to be unrelated to inhibition of neuronal uptake, block of alpha-adrenoceptors or stimulation of beta-adrenoceptors. Consequently, in addition to releasing noradrenaline, the scorpion toxin enhances transmitter overflow elicited by nerve stimulation through a prejunctional effect which appears to reflect a nove mechanism of action.
在先前用3H - 去甲肾上腺素标记的离体豚鼠心房中,研究了巴西蝎子Tityus serrulatus毒液的纯化组分的作用。暴露于0.3和1.0微克/毫升的蝎子毒素会产生持久的正性变时效应,且该效应呈浓度依赖性。心房率的增加与放射性物质自发流出的增强相吻合。暴露于1.0微克/毫升的蝎子毒素引起的放射性产物流出增加约3倍。3H - 去甲肾上腺素占蝎子毒素引起的放射性流出总量增加的60%,3H - 脱氨基二醇(3,4 - 二羟基苯乙二醇)是形成的主要代谢产物,约占总释放量的35%。暴露于1.0微克/毫升的蝎子毒素20分钟后,由加速神经刺激(4Hz,60秒超最大电压)引起的标记递质溢出增加了8倍。蝎子毒素的这种作用似乎与抑制神经元摄取、阻断α - 肾上腺素能受体或刺激β - 肾上腺素能受体无关。因此,除了释放去甲肾上腺素外,蝎子毒素还通过一种节前效应增强神经刺激引起的递质溢出,这似乎反映了一种新的作用机制。