Evaluation of anti-allergic effects of 1-substituted 2-n-butyl-methylenedioxy indenes.
The effects of ten 1-substituted 2-n-butyl-5,6-methylenedioxyindenes on mice and guinea pigs were investigated for their allergic reactions in the development of a new anti-allergic drug. Anti-allergic effects were determined by testing the effect of agents on passive cutaneous anaphylaxis (PCA) in mice and Schultz-Dale reaction in guinea pig tracheal muscle. 2-Butyl-1-[N-methyl-N-[2-(N',N'-dimethylamino) ethyl]amino]5,6- methylenedioxyindene (1) indicated the most potent anti-allergic activity. Since our previous experiments indicated that 2-n-butyl 3-dimethyl amino-5,6-methylenedioxyindene (MDI-A) and its derivatives showed a potent anti-allergic effect by interfering with the calcium (Ca) movement in the allergic reaction in guinea pigs, the effect of 1 and MDI-A on allergic reaction and Ca-induced contraction of tracheal muscle in these animals were compared. The present data indicate the superiority of 1 in both reactions.
Department of Pharmacology, Gifu Pharmaceutical University, Japan.
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H
Nagai
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Yakuo
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Hara
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Xu
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SH
Choi
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N
Inagaki
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A
Koda
D000818:Animals; D000941:Antigens / Q000276:immunology; D002122:Calcium Chloride / Q000494:pharmacology; D005260:Female; D006168:Guinea Pigs; D006632:Histamine / Q000494:pharmacology; D006967:Hypersensitivity / Q000188:drug therapy*; D007114:Immunization; D007192:Indenes / Q000494:pharmacology / Q000627:therapeutic use*; D008297:Male; D051379:Mice; D008925:Mites / Q000276:immunology; D015394:Molecular Structure; D009119:Muscle Contraction / Q000187:drug effects; D010323:Passive Cutaneous Anaphylaxis / Q000187:drug effects; D013189:SRS-A / Q000494:pharmacology; D014132:Trachea / Q000276:immunology / Q000502:physiology; D003189:p-Methoxy-N-methylphenethylamine / Q000494:pharmacology
D000941:Antigens; D007192:Indenes; D013189:SRS-A; C060698:2-butyl-1-(N-methyl-N-(2-(N',N'-dimethylamino)ethyl)amino)-5,6-methylenedioxyindene; D003189:p-Methoxy-N-methylphenethylamine; D006632:Histamine; D002122:Calcium Chloride