多巴胺能麦角碱衍生物的合成及其体外和体内评价

Synthesis and in vitro and in vivo evaluation of dopaminergic ergoline derivatives.

作者信息

Mantegani S, Brambilla E, Caccia C, Di Salle E, Cervini M A, McArthur R A, Traquandi G, Varasi M

机构信息

Pharmacia and Upjohn-CNS Research, Milan, Italy.

出版信息

Farmaco. 1998 Jan;53(1):65-72. doi: 10.1016/s0014-827x(97)00009-8.

DOI:10.1016/s0014-827x(97)00009-8

PMID:9543728

Abstract

A series of ergoline-amides was synthesised in the discovery of new dopaminomimetic agents. Several compounds exhibited in vivo high prolactin lowering activity (indirectly measured by the nidation test) in rats. For the most active, the potential anti-Parkinson activity was evaluated by observation of the contralateral turning behaviour in 6-OH-DA lesioned rats. The acute toxicity by oral route in mice was also studied.

摘要

在新型多巴胺模拟剂的研发过程中，合成了一系列麦角灵酰胺。几种化合物在大鼠体内表现出高催乳素降低活性（通过着床试验间接测量）。对于活性最高的化合物，通过观察6-羟基多巴胺损伤大鼠的对侧旋转行为来评估其潜在的抗帕金森活性。还研究了其对小鼠的口服急性毒性。