Martin G E, Williams M, Clineschmidt B V, Yarbrough G G, Jones J H, Haubrich D R
Life Sci. 1982 May 24;30(21):1847-56. doi: 10.1016/0024-3205(82)90323-x.
6-Ethyl-9-oxaergoline (EOE) and its enantiomers were compared with apomorphine in a number of tests designed to measure dopamine (DA) agonist activity within the central nervous system. In rats, the tests were: interaction with DA receptors labeled with 3H-apomorphine or 3H-spiroperidol; the effects on DA synthesis as assessed by the gamma-butyrolactone procedure; turning in 6-OHDA lesioned animals; stereotypy; and, slowing of DA cell firing rates. In the mouse, locomotor activity, hypothermia and postural asymmetry in caudectomized animals were studied. Emesis in the beagle was also examined. The (-)-enantiomer of EOE was more potent than either the (+)-enantiomer or the racemate in all tests. With the exception of inducing stereotypy and the displacement of 3H-apomorphine from rat striatal membranes, (-)-EOE was equi- or more potent than apomorphine in all test procedures. (-)-EOE was effective following oral administration and exhibited a longer duration of action than apomorphine. The results indicate EOE is a potent DA agonist.
在一系列旨在测量中枢神经系统内多巴胺（DA）激动剂活性的试验中，将6-乙基-9-氧杂麦角林（EOE）及其对映体与阿扑吗啡进行了比较。在大鼠中，试验包括：与用3H-阿扑吗啡或3H-螺哌啶醇标记的DA受体相互作用；通过γ-丁内酯程序评估对DA合成的影响；6-羟基多巴胺损伤动物的旋转行为；刻板行为；以及DA细胞放电速率的减慢。在小鼠中，研究了去尾动物的运动活性、体温过低和姿势不对称。还检查了比格犬的呕吐情况。在所有试验中，EOE的（-）-对映体比（+）-对映体或外消旋体更有效。除了诱导刻板行为和从大鼠纹状体膜上置换3H-阿扑吗啡外，（-）-EOE在所有试验程序中与阿扑吗啡等效或更有效。（-）-EOE口服给药有效，且作用持续时间比阿扑吗啡长。结果表明EOE是一种有效的DA激动剂。
