NAPHTHOSULTAM DERIVATIVES - A NEW CLASS OF POTENT AND SELECTIVE 5-HT2 ANTAGONISTS

被引：35

作者：

MALLERON, JL ^{[1
]}

COMTE, MT ^{[1
]}

GUEREMY, C ^{[1
]}

PEYRONEL, JF ^{[1
]}

TRUCHON, A ^{[1
]}

BLANCHARD, JC ^{[1
]}

DOBLE, A ^{[1
]}

PIOT, O ^{[1
]}

ZUNDEL, JL ^{[1
]}

HUON, C ^{[1
]}

MARTIN, B ^{[1
]}

MOUTON, P ^{[1
]}

VIROULAUD, A ^{[1
]}

ALLAM, D ^{[1
]}

BETSCHART, J ^{[1
]}

机构：

[1] CTR RECH VITRY ALFORTVILLE RHONE POULENC RORER,DEPT BIOL,F-94403 VITRY,FRANCE

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 1991年 / 34卷 / 08期

关键词：

D O I：

10.1021/jm00112a025

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-(aminoalkyl)naphth[1,8-cd]isothiazole 1,1-dioxides was synthesized and examined in various receptor binding tests. Most compounds demonstrated high affinity for the 5-HT2 receptor with moderate to high selectivity. A member of this series, compound 24 (RP 62203), displays high 5-HT2 receptor affinity (K(i) = 0.26 nM), which is respectively more than 100 and 1000 times higher than its affinity for alpha-1 (K(i) = 38 nM) and D2 (K(i) > 1000 nM) receptors. This compound is a potent orally effective and long lasting 5-HT2 antagonist in the mescaline-induced head-twitches test in mice and rats.

引用

页码：2477 / 2483

页数：7

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