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.
MeSH terms
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Adrenocorticotropic Hormone / metabolism
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Animals
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Carboxylic Acids / chemical synthesis*
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Carboxylic Acids / pharmacology
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Cells, Cultured
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Cyclic AMP / metabolism
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Humans
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Male
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Pituitary Gland / drug effects*
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Pituitary Gland / metabolism
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Quinazolines / chemical synthesis*
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Quinazolines / pharmacology
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Rats
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Receptors, Corticotropin-Releasing Hormone / antagonists & inhibitors*
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Transfection
Substances
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Carboxylic Acids
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Quinazolines
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Receptors, Corticotropin-Releasing Hormone
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oxo-7H-benzo(e)perimidine-4-carboxylic acid
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Adrenocorticotropic Hormone
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Cyclic AMP