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ID: ALA1132065
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists.
Authors: Luthin DR, Rabinovich AK, Bhumralkar DR, Youngblood KL, Bychowski RA, Dhanoa DS, May JM.
Abstract: A novel series of derivatives of oxo-7H-benzo[e]perimidine-4-carboxylic acid (I) potently displaced radioligand binding of 125I-CRF to both CRF1 and CRF2 receptors. The members of this series antagonized CRF-stimulated cAMP formation and CRF-stimulated corticotropin release from rat pituitary in vivo. These are the first nonpeptide antagonists to show activity at both CRF1 and CRF2 receptors.
CiteXplore: 10201844