Abstract
Dimethindene maleate (Fenistil®), an, H1-receptor blocker, exists in the form of two enantiomers: S-(−)-dimethindene maleate and R-(+)-dimethindene maleate. These two enantiomers were tested for their antihistaminic and anti-anaphylactic properties in guinea-pigs. The S-enantiomer was much more active than the R-enantiomer. The ED50 for protection against a standard lethal dose of histamine 3 h after S-(−)-dimethindene maleate application was 0.056 mg/kg b.w. p.o. and against fatal anaphylactic shock 0.273 mg/kg b.w. p.o. Values of 14.32 mg/kg b.w. p.o. and >31.6 mg/kg b.w. p.o. were determined for the R-(+)-enantiomer.
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