8-(4-Methoxyphenyl) pyrazolo [1, 5-a]-1, 3, 5-triazines: selective and centrally active corticotropin-releasing factor receptor-1 (CRF1) antagonists

…, L He, T Clarke, P Tivitmahaisoon, S Lelas…

文献索引：Gilligan, Paul J.; He, Liqi; Clarke, Todd; Tivitmahaisoon, Parcharee; Lelas, Snjezana; Li, Yu-Wen; Heman, Karen; Fitzgerald, Lawrence; Miller, Keith; Zhang, Ge; Marshall, Anne; Krause, Carol; McElroy, John; Ward, Kathyrn; Shen, Helen; Wong, Harvey; Grossman, Scott; Nemeth, Gregory; Zaczek, Robert; Arneric, Stephen P.; Hartig, Paul; Robertson, David W.; Trainor, George Journal of Medicinal Chemistry, 2009 , vol. 52, # 9 p. 3073 - 3083

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被引用次数: 23

摘要

This report describes the syntheses and structure− activity relationships of 8-(4- methoxyphenyl) pyrazolo [1, 5-a]-1, 3, 5-triazine corticotropin releasing factor receptor-1 (CRF1) receptor antagonists. CRF1 receptor antagonists may be potential anxiolytic or antidepressant drugs. This research culminated in the discovery of analogue 12-3, which is a potent, selective CRF1 antagonist (hCRF1 IC50= 4.7±2.0 nM) with weak affinity for the ...