Title of article
Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 1999
Pages
6
From page
765
To page
770
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.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
1999
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790033
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