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 D R Rabinovich A K Bhumralkar D R Youngblood K L Bychowski R A Dhanoa D S May J M |
| |
Affiliation: | Alanex Corporation, A Subsidiary of Agouron Pharmaceuticals, Inc., San Diego, CA 92121, USA. |
| |
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. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |