THE CENTRAL LOCOMOTOR STIMULATORY ACTIVITY AND ACUTE TOXICITY OF THE EPHEDRINE AND NOREPHEDRINE ISOMERS IN MICE

¹ Department of Pharmacology, University of California, Los Angeles, and Veterans Administration Hospital, Long Beach, California

The entire series of ephedrine and norephedrine optical isomers were compared in mice for their acute toxicity and central locomotor stimulatory activity. The optical isomers of amphetamine were included as reference compounds. Clear central locomotor stimulation was produced by five of the 10 compounds in the test series. With the most potent compound, d-amphetamine, given a value of 1.0, the following activity ratios were observed: l-amphetamine, 4; d-norpseudoephedrine, 10; l-ephedrine, 24; and l-norpseudoephedrine, 43. The compounds l-norephedrine, d-norephedrine, l-pseudoephedrine, d-pseudoephedrine and d-ephedrine produced measurable locomotor stimulation only in doses approaching lethal amounts. The relationship between central stimulant potency and molecular structure is discussed.

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