Biochemical Pharmacology 1986-12-15

Tissue levels and some in vivo responses to a monofluorinated analogue of amphetamine in the mouse.

T J Danielson, R Keashly, R T Coutts

Index: Biochem. Pharmacol. 35(24) , 4423-9, (1986)

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Abstract

The metabolism and some behavioral properties of each of the optical isomers of 2-amino-1-fluoro-3-phenylpropane hydrochloride (fluoroamphetamine, FAM) were examined and compared to those of the optical isomers of amphetamine (AM). Substitution of fluorine into the side-chain of AM increased the rate of elimination of drug from brain and modified the kinetics from a one- to a two-compartment model. Urinary excretion of unchanged S-(-)-FAM was reduced from that observed after R-(-)-AM, suggesting a more extensive metabolism. Fluorine substitution also modified the behavioral response to AM. Thus, each optical isomer of FAM produced paradoxical reductions in locomotor activity and body temperature.