Pyrazolo-[1, 5-a]-1, 3, 5-triazine corticotropin-releasing factor (CRF) receptor ligands

…, S Andreuski, L Fitzgerald, K Miller, WJ Marshall

Index: Gilligan, Paul J.; Folmer, Beverly K.; Hartz, Richard A.; Koch, Stephanie; Nanda, Kausik K.; Andreuski, Stephen; Fitzgerald, Lawrence; Miller, Keith; Marshall, William J. Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 18 p. 4093 - 4102

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Citation Number: 18

Abstract

The syntheses and rat CRF receptor binding affinities of 'retro-pyrazolotriazine'corticotropin- releasing factor (CRF) ligands 4 are reported. Some have high affinity for rat CRF receptors (Ki≤ 10 nM). The data provide additional support for the hypothesis that it is possible to interchange isosteric cores with similar electronic properties in the design of high-affinity CRF receptor ligands, provided the peripheral pharmacophore elements are maintained ...