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Journal of Pharmacology And Experimental Therapeutics, Vol. 93, Issue 3, 282-286, 1948
Copyright © 1948 by American Society for Pharmacology and Experimental Therapeutics

PHARMACOLOGIC COMPARISON OF THE OPTICAL ISOMERS OF METHADON

C. C. Scott 1, E. B. Robbins 1, and K. K. Chen 1

1 The Lilly Research Laboratories, Eli Lilly and Company, Indianapolis 6, Indiana

1. The analgesic action of l-Dolophine is much greater than that of the d-isomer, the order of activity being approximately 7.5:1 in rats, 25:1 in dogs, and 50:1 in man.

2. l-Dolophine produces more narcosis than the d-form in equianalgesic doses.

3. In anesthetized dogs, l-Dolophine is 25 times as depressant to respiration, but 65 times as stimulating to duodenum, as the d-isomer.

4. There is little difference in toxicity between the l- and d-isomers in mice by intravenous injection. Either optical isomer is, however, slightly less toxic than the racemic mixture.

Submitted on March 6, 1948




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Copyright © 1948 by the American Society for Pharmacology and Experimental Therapeutics.