Gianutsos G, Moore K E
Psychopharmacology (Berl). 1980;68(2):139-46. doi: 10.1007/BF00432131.
Some behavioral and biochemical effects of four dopaminergic agonists (apomorphine, piribedil, lergotrile, and bromocriptine) were determined in the mouse. As expected, all four drugs dose-dependently reversed the alpha-methyltyrosine-induced decline of forebrain dopamine. All four compounds reduced locomotor activity at low doses, but only apomorphine and bromocriptine increased motor activity at higher doses. All four drugs caused some reversal of the baclofen-induced elevation in forebrain dopamine concentrations, but only apomorphine and bromocriptine completely reversed the effects of baclofen. After chronic treatment with haloperidol, the behavioral effects of lergotrile and bromocriptine were altered. Doses of those drugs reducing motor activity in normal animals were ineffective after chronic haloperidol. The latent stimulation induced by bromocriptine was enhanced, while a stimulatory effect of lergotrile emerged in these animals. These effects were noted in conjunction with an enhanced sensitivity to the drug-induced decrease in dopamine turnover. These results demonstrate that dopamine agonists may be differentiated on the basis of certain behavioral and biochemical tests and suggest an interaction of these drugs with two different populations of dopamine receptors.
研究了四种多巴胺能激动剂（阿扑吗啡、吡贝地尔、麦角腈和溴隐亭）对小鼠的一些行为和生化影响。正如预期的那样，所有四种药物均呈剂量依赖性地逆转了α-甲基酪氨酸诱导的前脑多巴胺水平下降。所有四种化合物在低剂量时均降低了运动活性，但只有阿扑吗啡和溴隐亭在高剂量时增加了运动活性。所有四种药物都使巴氯芬诱导的前脑多巴胺浓度升高有所逆转，但只有阿扑吗啡和溴隐亭完全逆转了巴氯芬的作用。用氟哌啶醇长期治疗后，麦角腈和溴隐亭的行为效应发生了改变。在正常动物中降低运动活性的那些药物剂量，在长期使用氟哌啶醇后变得无效。溴隐亭诱导的潜在刺激作用增强，而在这些动物中麦角腈出现了刺激作用。这些效应与对药物诱导的多巴胺周转减少的敏感性增强有关。这些结果表明，多巴胺激动剂可以根据某些行为和生化测试进行区分，并提示这些药物与两种不同类型的多巴胺受体存在相互作用。
