Synthesis and structure–activity relationships of pyrido [3, 2-b] pyrazin-3 (4H)-ones and pteridin-7 (8H)-ones as corticotropin-releasing factor-1 receptor antagonists

…, AG Takvorian, M Rafalski, P Kasireddy-Polam…

Index: Dzierba, Carolyn D.; Sielecki, Thais M.; Arvanitis, Argyrios G.; Galka, Amy; Johnson, Tricia L.; Takvorian, Amy G.; Rafalski, Maria; Kasireddy-Polam, Padmaja; Vig, Shikha; Dasgupta, Bireshwar; Zhang, Ge; Molski, Thaddeus F.; Wong, Harvey; Zaczek, Robert C.; Lodge, Nicholas J.; Combs, Andrew P.; Gilligan, Paul J.; Trainor, George L.; Bronson, Joanne J.; MacOr, John E. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 15 p. 4986 - 4989

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Abstract

Corticotropin Releasing Factor (CRF), a 41 amino acid peptide first isolated in 1981, 1 is considered to be one of the principal regulators of the hypothalamic–pituitary–adrenal (HPA) axis, which coordinates the endocrine, behavioral and autonomic responses to stress. CRF mediates its action through binding to two well characterized, class B subtype G-protein coupled receptors, CRF-R1 and CRF-R2, which are widely distributed throughout the central and ...