Tissue levels and some in vivo responses to a monofluorinated analogue of amphetamine in the mouse.
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.
D000662:Amphetamines / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D001831:Body Temperature / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D005260:Female; D007700:Kinetics; D008297:Male; D051379:Mice; D009043:Motor Activity / Q000187:drug effects; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
D000662:Amphetamines; C040639:4-fluoroamphetamine