Author/Authors :
David R. Luthin، نويسنده , , Aleksandr K. Rabinovich، نويسنده , , Dilip R. Bhumralkar، نويسنده , , Kenna L. Youngblood، نويسنده , , Richard A. Bychowski، نويسنده , , Daljit S. Dhanoa، نويسنده , , John M. May، نويسنده ,
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.
