Gong J P, Gwee M C, Gopalakrishnakone P
Department of Anatomy, Faculty of Medicine, National University of Singapore, Singapore.
Toxicon. 1995 Sep;33(9):1133-9. doi: 10.1016/0041-0101(95)00053-o.
The effect of Buthus martensi Karsch venom (MKV) on adrenergic responses was investigated using the rat isolated anococcygeus muscle (Acm), since several scorpion venoms can cause peripheral sympathetic nerve stimulation with enhanced adrenergic responses. The effects of phentolamine (5 microM), guanethidine (5 microM), tetrodotoxin (2 microM), desipramine (1.5 microM) and reserpine pretreatment in vivo (5 mg/kg s.c. x 24 hr and 5 mg/kg i.p. x 3 hr) on contractile responses of the rat Acm to field stimulation, noradrenaline (3 microM), tyramine (10 microM), crude MKV (2 micrograms/ml), carbachol (3 microM) and potassium chloride (50 mM) were compared. Phentolamine, guanethidine, tetrodotoxin and reserpine pretreatment completely blocked the contractile responses of the Acm to MKV and to field stimulation but desipramine potentiated the responses. The responses to NA were completely blocked by phentolamine, but were potentiated by guanethidine, desipramine and reserpine pretreatment. The contractile responses to tyramine were completely blocked by phentolamine, desipramine and reserpine pretreatment. The low doses (0.1 microgram/ml x 3) of MKV, which did not produce any observable increase in tone of the anococcygeus muscle, potentiated the contractile responses to field stimulation, but not the responses to exogenous NA. Thus, the adrenergic agonist action of MKV in the rat isolated anococcygeus muscle is mediated by some prejunctional mechanism(s) of action, presumably stimulating the release of the neurotransmitter noradrenaline.
由于几种蝎毒可引起外周交感神经兴奋并增强肾上腺素能反应,因此使用大鼠离体肛门尾骨肌(Acm)研究了东亚钳蝎毒(MKV)对肾上腺素能反应的影响。比较了酚妥拉明(5 microM)、胍乙啶(5 microM)、河豚毒素(2 microM)、地昔帕明(1.5 microM)和体内利血平预处理(5 mg/kg皮下注射×24小时和5 mg/kg腹腔注射×3小时)对大鼠Acm对场刺激、去甲肾上腺素(3 microM)、酪胺(10 microM)、粗制MKV(2微克/毫升)、卡巴胆碱(3 microM)和氯化钾(50 mM)的收缩反应的影响。酚妥拉明、胍乙啶、河豚毒素和利血平预处理完全阻断了Acm对MKV和场刺激的收缩反应,但地昔帕明增强了这些反应。对去甲肾上腺素的反应被酚妥拉明完全阻断,但被胍乙啶、地昔帕明和利血平预处理增强。对酪胺的收缩反应被酚妥拉明、地昔帕明和利血平预处理完全阻断。低剂量(0.1微克/毫升×3)的MKV不会使肛门尾骨肌张力出现任何明显增加,它增强了对场刺激的收缩反应,但未增强对外源性去甲肾上腺素的反应。因此,MKV在大鼠离体肛门尾骨肌中的肾上腺素能激动剂作用是由某些节前作用机制介导的,可能是刺激了神经递质去甲肾上腺素的释放。