SYNTHESIS AND ORAL EFFICACY OF A 4-(BUTYLETHYLAMINO)PYRROLO[2,3-D]PYRIMIDINE - A CENTRALLY ACTIVE CORTICOTROPIN-RELEASING FACTOR(1) RECEPTOR ANTAGONIST

Authors
CHEN YL MANSBACH RS WINTER SM BROOKS E COLLINS J CORMAN ML DUNAISKIS AR FARACI WS GALLASCHUN RJ SCHMIDT A SCHULZ DW
Citation
Yl. Chen et al., SYNTHESIS AND ORAL EFFICACY OF A 4-(BUTYLETHYLAMINO)PYRROLO[2,3-D]PYRIMIDINE - A CENTRALLY ACTIVE CORTICOTROPIN-RELEASING FACTOR(1) RECEPTOR ANTAGONIST, Journal of medicinal chemistry, 40(11), 1997, pp. 1749-1754
Citations number
24
Categorie Soggetti
Chemistry Medicinal
Journal title
Journal of medicinal chemistry → ACNP
ISSN journal
00222623
Volume
40
Issue
11
Year of publication
1997
Pages
1749 - 1754
Database
ISI
SICI code
0022-2623(1997)40:11<1749:SAOEOA>2.0.ZU;2-A
Abstract
The syntheses of a centrally active nonpeptide CRF1 receptor antagonis t 2, ethylphenyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl]amine (CP-154,526), and its analogs 11-14 and [H-3]-2 are reported. The in vitro CRF1 rece ptor binding affinity in the series 2, the pharmacokinetic properties of 2 in rats, and the anxiolytic-like effects of orally administered 2 are presented.