JPET Celsis microsomes equal better data

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Journal of Pharmacology And Experimental Therapeutics, Vol. 103, Issue 4, 306-309, 1951
Copyright © 1951 by American Society for Pharmacology and Experimental Therapeutics


THE TOPICAL ANESTHETIC ACTIVITY OF AN ISOQUINOLINE COMPOUND

Edwin J. Fellows 1 and Edward Macko 1

1 Research and Development Division, Smith, Kline and French Laboratories, Philadelphia, Pennsylvania

1. When applied to rabbit eyes, 1-(beta-dimethylaminoethoxy)-3-butylisoquinoline monohydrochloride (Quotane) was found to be 1000 times more active than cocaine and ten times more potent than dibucaine.

2. Intraperitoneally in rats Quotane was 50 per cent less toxic than dibucaine and twice as toxic as cocaine.

3. Intravenously in rabbits Quotane was one-half as toxic as dibucaine.

4. While the intradermal potency of Quotane did not parallel its topical effectiveness it was nevertheless found to be 100 times more active than procaine.

5. Massive doses of Quotane were administered daily to rats and guinea pigs without producing histopathologically demonstrable tissue damage.

Submitted on August 7, 1951







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Copyright © 1951 by the American Society for Pharmacology and Experimental Therapeutics.