首页 | 本学科首页   官方微博 | 高级检索  
     


Potent dopamine agonist activity of a novel ergoline, 6-Ethyl-9-oxaergoline (EOE)
Authors:G.E. Martin  M. Williams  B.V. Clineschmidt  G.G. Yarbrough  J.H. Jones  D.R. Haubrich
Affiliation:Merck Sharp & Dohme Research Laboratories West Point, Pennsylvania 19486, USA
Abstract: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
/></figure>-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 <sup>3</sup>H-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.</td> </tr> <tr> <td align=
Keywords:
本文献已被 ScienceDirect 等数据库收录！
设为首页 | 免责声明 | 关于勤云 | 加入收藏

Copyright©北京勤云科技发展有限公司  京ICP备09084417号