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Proposed dopaminergic pharmacophore of lergotrile, pergolide, and related ergot alkaloid derivatives

JG Cannon, BJ Demopoulos, JP Long…

文献索引:Cannon; Demopoulos; Long; Flynn; Sharabi Journal of Medicinal Chemistry, 1981 , vol. 24, # 3 p. 238 - 240

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被引用次数: 56

摘要

10 and dopamine binding, which are characteristic actions of dopaminergic agonists. Bach et al. ll found that 3-(2-aminoethy1) pyrrole (7) was ineffective in lowering prolactin levels, which was attributed to rapid metabolic inactivation of the primary amine by monoamine oxidase. No tertiary amine derivative of 7 was reported. Compound 8, a BC bicyclic ergoline partial structure, exhibited prolactin inhibitory activity, as well as some activity in a rat ...