Williams P D, Bendele A, Deldar A, McGrath J, Shetler T, Owen N
Lilly Research Laboratories, Eli Lilly and Company, Greenfield, Indiana.
Arzneimittelforschung. 1992 Jul;42(7):891-5.
Pergolide mesylate ((8 beta)-8-[(methylthio)methyl]-6-propylergoline monomethanesulfonate, LY 127809, CAS 66104-23-2) is a novel and potent dopamine agonist marketed for treating the symptoms of Parkinson's disease. The potential secondary pharmacological effects of this agent on the gastrointestinal and renal systems, as well as effects on local anesthesia, hemolysis, platelet aggregation, circulating blood glucose, primary antibody production, and the acute inflammatory response were examined. Pergolide exhibited significant pharmacological effects in gastrointestinal, renal and anti-inflammatory tests at high oral doses. Pergolide was essentially inactive in blood hemolysis, platelet aggregation, primary antibody production and local anesthesia testing. In summary, these studies confirm the pharmacological selectivity of pergolide, and indicate a low potential for secondary pharmacological side effects upon the functions tested at clinically relevant doses.
甲磺酸培高利特((8β)-8-[(甲硫基)甲基]-6-丙基麦角林单甲磺酸盐,LY 127809,CAS 66104-23-2)是一种新型强效多巴胺激动剂,用于治疗帕金森病症状。研究了该药物对胃肠和肾脏系统的潜在次要药理作用,以及对局部麻醉、溶血、血小板聚集、循环血糖、初次抗体产生和急性炎症反应的影响。高口服剂量时,培高利特在胃肠、肾脏和抗炎试验中表现出显著药理作用。培高利特在血液溶血、血小板聚集、初次抗体产生和局部麻醉试验中基本无活性。总之,这些研究证实了培高利特的药理选择性,并表明在临床相关剂量下,对所测试功能产生次要药理副作用的可能性较低。