Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4- carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists

Article abstract of DOI:10.1016/S0960-894X(99)00075-X

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.