Krejci I, Schuh J, Prágerová H, Dlabac A
Pol J Pharmacol Pharm. 1985 May-Jun;37(3):263-71.
The effects of apomorphine, lisuride and 9, 10 transdihydrolisuride (TDHL) were compared on two models of rotating rat. In rats with 6-hydroxydopamine (6OHDA) induced unilateral lesions, all three drugs evoked contralateral rotation. By contrast, in rats with unilateral electrolytical lesions of the striatum, only apomorphine and lisuride acted as agonists. TDHL did not cause any circling and inhibited rotation induced by apomorphine and lisuride. In other experiments the effects on body temperature was examined. All three drugs lowered the rectal temperature in normal mice; however, only apomorphine and--to some extent--lisuride reversed the hypothermia induced by reserpine. Both lisuride and TDHL inhibited the hypothermia reversal induced by apomorphine. The presented results are interpreted in terms of lower intrinsic activities of TDHL and lisuride in comparison with apomorphine. The lower intrinsic activity is manifested as partial agonist or antagonist type of action in dependence on the location and the state of receptors.
在两种旋转大鼠模型上比较了阿扑吗啡、利苏瑞ide和9,10-反式二氢利苏瑞ide(TDHL)的作用。在6-羟基多巴胺(6OHDA)诱导的单侧损伤大鼠中,这三种药物均引起对侧旋转。相比之下,在纹状体单侧电解损伤的大鼠中,只有阿扑吗啡和利苏瑞ide起激动剂作用。TDHL不引起任何旋转,并抑制阿扑吗啡和利苏瑞ide诱导的旋转。在其他实验中,检测了对体温的影响。这三种药物均降低正常小鼠的直肠温度;然而,只有阿扑吗啡以及在一定程度上利苏瑞ide能逆转利血平诱导的体温过低。利苏瑞ide和TDHL均抑制阿扑吗啡诱导的体温过低逆转。与阿扑吗啡相比,TDHL和利苏瑞ide的内在活性较低,据此对所呈现的结果进行了解释。较低的内在活性根据受体的位置和状态表现为部分激动剂或拮抗剂类型的作用。