Borsy J
Pol J Pharmacol Pharm. 1985 May-Jun;37(3):227-36.
Recently, the importance of the dopamine receptor agonists has increased in the treatment of parkinsonism, different endocrinological diseases and cardiovascular illness. In the therapy some well known drugs, derivatives of ergot groups e.g. bromocriptine, lisuride and pergolide, have been found useful. In the Institute for Drug Research numerous semi-synthetic elymoclavine derivatives were synthesized during the past years, and the influence of these new compounds on both the central and peripheral dopamine transmission was examined. Among the different ergot derivatives compound GYKI-32 887 seemed to be the most effective dopamine agonist and it was selected for preclinical investigation. The endocrinological effects and the pre- and postsynaptic dopamine receptor stimulant activity of this new compound are summarized. GYKI-32 887 was more potent than bromocriptine as regards its inhibitory effect on prolactin secretion and antiparkinsonian efficacy. Besides the strong dopamine receptor stimulant action this new ergoline compound, contrary to bromocriptine, inhibits the convulsive action of bicucullin. It may be assumed that the GABA receptor agonistic effect of GYKI-32 887 would be also valuable in the treatment of various form of dyskinesias.
最近，多巴胺受体激动剂在帕金森病、不同内分泌疾病及心血管疾病的治疗中愈发重要。在治疗中，一些知名药物，如麦角类衍生物溴隐亭、利舒脲和培高利特，已被证实有效。在药物研究所，过去几年合成了众多半合成麦角新碱衍生物，并研究了这些新化合物对中枢及外周多巴胺传递的影响。在不同的麦角衍生物中，化合物GYKI-32 887似乎是最有效的多巴胺激动剂，并被选用于临床前研究。本文总结了这种新化合物的内分泌作用以及突触前和突触后多巴胺受体刺激活性。就其对催乳素分泌的抑制作用和抗帕金森病疗效而言，GYKI-32 887比溴隐亭更有效。除了强大的多巴胺受体刺激作用外，与溴隐亭不同，这种新的麦角灵化合物还能抑制荷包牡丹碱的惊厥作用。可以推测，GYKI-32 887的GABA受体激动作用在治疗各种形式的运动障碍中也可能具有重要价值。
