Interaction of pergolide with central dopaminergic receptors

摘要: Abstract The activity of pergolide, an N-propylergoline derivative, has been tested for stimulation central dopaminergic receptors. Binding to dopamine receptors shows that pergolide acts as agonist with respect these GTP decreases the potencies agonists and but not bromocriptine, displace [3H]spiroperidol ([3H]Spi) from striatal membrane sites. The GTP-sensitive site labeled by [3H]Spi seems be localized on intrastriatal potency receptor sites is reduced in membranes exposed higher temperatures. Pergolide, hitherto-tested ergots, stimulates dopamine-sensitive adenylate cyclase homogenates. Thus, unlike other components binding linked cyclase. drug also induces turning behavior rats 6-OH-dopamine lesions relieves tremor monkeys ventromedial tegmental a longer time at lower dose than ergots. Other studies have shown it effective treatment patients advanced parkinsonism.