CALCIUM-INDEPENDENT PHOSPHODIESTERASE INHIBITORS AS PUTATIVE ANTIDEPRESSANTS - [3-(BICYCLOALKYLOXY)-4-METHOXYPHENYL]-2-IMIDAZOLIDINONES

被引:42
作者
SACCOMANO, NA
VINICK, FJ
KOE, BK
NIELSEN, JA
WHALEN, WM
MELTZ, M
PHILLIPS, D
THADIEO, PF
JUNG, S
CHAPIN, DS
LEBEL, LA
RUSSO, LL
HELWEG, DA
JOHNSON, JL
IVES, JL
WILLIAMS, IH
机构
[1] Central Research, Pfizer Inc., Groton
关键词
D O I
10.1021/jm00105a045
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis and biological properties of a novel series of selective calcium-independent phosphodiesterase inhibitors are described. These compounds also inhibit the specific binding of [H-3]rolipram to rat brain membranes and exhibit efficacy in preclinical models of antidepressant activity in mice, such as reducing immobility in the forced-swim test and reversing reserpine-induced hypothermia. Imidazolidinones 4 and 16 were found to be the most potent compounds studied.
引用
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页码:291 / 298
页数:8
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