Synthesis and oral efficacy of a 4-(butylethylamino)pyrrolo[2,3-d]pyrimidine: A centrally active corticotropin-releasing factor(1) receptor antagonist

被引：111

作者：

Chen, YL ^{[1
]}

Mansbach, RS ^{[1
]}

Winter, SM ^{[1
]}

Brooks, E ^{[1
]}

Collins, J ^{[1
]}

Corman, ML ^{[1
]}

Dunaiskis, AR ^{[1
]}

Faraci, WS ^{[1
]}

Gallaschun, RJ ^{[1
]}

Schmidt, A ^{[1
]}

Schulz, DW ^{[1
]}

机构：

[1] PFIZER INC,DIV CENT RES,DEPT NEUROSCI,GROTON,CT 06340

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1997年 / 40卷 / 11期

关键词：

D O I：

10.1021/jm960861b

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 [H-3]-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.

引用

页码：1749 / 1754

页数：6

共 24 条

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