Dr. Luthin et al., Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists, BIOORG MED, 9(5), 1999, pp. 765-770
A novel series of derivatives of oxo-7H-benzo[e]perimidine-4-carboxylic aci
d (I) potently displaced radioligand binding of I-125-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 vi
vo. These are the first nonpeptide antagonists to show activity at both CRF
1 and CRF2 receptors. (C) 1999 Elsevier Science Ltd. All rights reserved.