
Bioorganic and Medicinal Chemistry Letters p. 765 - 770 (1999)
Update date:2022-08-03
Topics:
Luthin, David R.
Rabinovich, Aleksandr K.
Bhumralkar, Dilip R.
Youngblood, Kenna L.
Bychowski, Richard A.
Dhanoa, Daljit S.
John M, May
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.
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