Synthesis and biological activity of oxo-7H-benzo[e]perimidine-4-carboxylic acid derivatives as potent, nonpeptide corticotropin releasing factor (CRF) receptor antagonists |
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| Authors: | Luthin D R Rabinovich A K Bhumralkar D R Youngblood K L Bychowski R A Dhanoa D S May J M |
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| Institution: | Alanex Corporation, A Subsidiary of Agouron Pharmaceuticals, Inc., San Diego, CA 92121, USA. |
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| Abstract: | A novel series of derivatives of oxo-7H-benzoe]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. |
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