Walters J R, Lakoski J M, Baring M D, Eng N
Eur J Pharmacol. 1979 Dec 7;60(2-3):199-210. doi: 10.1016/0014-2999(79)90219-x.
Intravenous administration of increasing doses of the ergoline, lergotrile mesylate, caused a rapid, dose-dependent and haloperidol-reversible inhibition of unit activity of dopamine cells in the pars compacta of the rat substantia nigra. 6 microgram/kg caused significant depression of dopamine cell firing rates; 50% inhibition was achieved with a cumulative dose of 100 microgram/kg. 60% of the cells were completely inhibited by increasing doses of the drug, the remainder became resistant to further inhibition after reaching rates 25--50% of baseline. Pretreatment with reserpine and alpha-methylparatyrosine did not significantly attenuate the lergotrile-induced inhibition. Lergotrile had no consistent effect on firing rates of cells in the pars reticulata of the substantia nigra. The ergoline reduced the apparent activation of striatal dopamine synthesis associated with complete cessation of impulse flow in nigral-striatal dopamine neurons induced by gamma-butyrolactone treatment. These effects are compared with those of apomorphine and amphetamine. The results are consistent with the idea that lergotrile is a direct acting dopamine agonist.
静脉注射递增剂量的麦角灵甲磺酰麦角腈，会导致大鼠黑质致密部多巴胺能细胞单位活动迅速出现剂量依赖性且可被氟哌啶醇逆转的抑制。6微克/千克可使多巴胺能细胞放电率显著降低；累积剂量达100微克/千克时，抑制率达到50%。随着药物剂量增加，60%的细胞被完全抑制，其余细胞在放电率降至基线的25%至50%后，对进一步抑制产生抗性。用利血平和α-甲基对酪氨酸预处理并不能显著减弱甲磺酰麦角腈诱导的抑制作用。甲磺酰麦角腈对黑质网状部细胞的放电率没有一致的影响。麦角灵降低了与γ-丁内酯处理诱导的黑质纹状体多巴胺神经元冲动流完全停止相关的纹状体多巴胺合成的明显激活。将这些效应与阿扑吗啡和苯丙胺的效应进行了比较。结果与甲磺酰麦角腈是一种直接作用的多巴胺激动剂这一观点一致。
