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Pyrroloisoquinoline antidepressants. 2. In-depth exploration of structure-activity relationships

BE Maryanoff, DF McComsey, JF Gardocki…

文献索引:Maryanoff; McComsey; Gardocki; Shank; Costanzo; Nortey; Schneider; Setler Journal of Medicinal Chemistry, 1987 , vol. 30, # 8 p. 1433 - 1454

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被引用次数: 152

摘要

A series of pyrrolo [2, 1-a] isoquinolines, and related compounds, were examined for antidepressant-like activity, by virtue of their antagonism of tetrabenazine-induced ptosis and sedation, and inhibition of biogenic amine uptake. Thus, we have identified some of the most potent antagonists of TBZ-induced ptosis and some of the most potent inhibitors of the uptake of dopamine, norepinephrine, and serotonin (in rat brain synaptosomes) ever ...