Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: a centrally active corticotropin-releasing factor1 receptor antagonist.

Autor: Chen YL; Medicinal Chemistry Department, Pfizer Inc., Groton, Connecticut 06340, USA. yuhpyng_l_chen@groton.pfizer.com., Mansbach RS, Winter SM, Brooks E, Collins J, Corman ML, Dunaiskis AR, Faraci WS, Gallaschun RJ, Schmidt A, Schulz DW
Jazyk: angličtina
Zdroj: Journal of medicinal chemistry [J Med Chem] 1997 May 23; Vol. 40 (11), pp. 1749-54.
DOI: 10.1021/jm960861b
Abstrakt: 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.
Databáze: MEDLINE