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J Med Chem. 1991 Aug;34(8):2477-83.

Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists.

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  • 1Département de Chimie Pharmaceutique, Centre de Recherches de Vitry Alfortville Rhône-Poulenc Rorer, Vitry-sur-Seine, France.


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 (Ki = 0.26 nM), which is respectively more than 100 and 1000 times higher than its affinity for alpha 1 (Ki = 38 nM) and D2 (Ki greater than 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.

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