Chromeno [3, 4-c] pyridin-5-ones: selective human dopamine D4 receptor antagonists as potential antipsychotic agents

…, DT Connor, TG Heffner, RG MacKenzie…

文献索引：Unangst, Paul C.; Capiris, Thomas; Connor, David T.; Heffner, Thomas G.; MacKenzie, Robert G.; Miller, Steven R.; Pugsley, Thomas A.; Wise, Lawrence D. Journal of Medicinal Chemistry, 1997 , vol. 40, # 17 p. 2688 - 2693

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被引用次数: 67

摘要

The discovery of a series of chromeno [3, 4-c] pyridin-5-ones with selective affinity for the dopamine D4 receptor is described. Target compounds were tested for binding to cloned human dopamine D2, D3, and D4 receptor subtypes expressed in Chinese hamster ovary (CHO) K-1 cells. Several compounds demonstrated single digit nanomolar K i values for binding to the D4 receptor with several hundred-fold selectivities toward the D2 and D3 ...