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Synthesis and Oral Efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a Centrally Active Corticotropin-releasing Factor1 Receptor Antagonist

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Journal J Med Chem
Specialty Chemistry
Date 1997 May 23
PMID 9171885
Citations 15
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Abstract

The syntheses of a centrally active nonpeptide CRF1 receptor antagonist 2, butylethyl[2,5-dimethyl-7-(2,4,6-trimethylphenyl)-7H-pyrrolo [2,3-d]pyrimidin-4-yl]amine (CP-154,526), and its analogs 11-14 and [3H]-2 are reported. The in vitro CRF1 receptor binding affinity in the series 2, the pharmacokinetic properties of 2 in rats, and the anxiolytic-like effects of orally administered 2 are presented.

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