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Comparison of 4-chloro-, 4-bromo- and 4-fluoroamphetamine in rats: drug levels in brain and effects

Comparison of 4-chloro-, 4-bromo- and 4-fluoroamphetamine in rats: drug levels in brain and effects

  1. babymakesbeats
    Comparison of 4-chloro-, 4-bromo- and 4-fluoroamphetamine in rats: drug levels in brain and effects on brain serotonin metabolism.
    Neuropharmacology. 1975 Oct;14(10):739-46.
    Fuller RW, Baker JC, Perry KW, Molloy BB.

    Summary-The ability of 4-chjo~oamphetamine, 4-bromoamphetamine, and 4-fluoroampheta-
    mine to deplete brain S-hydroxyindoles and some pharmacokinetic properties of these drugs
    were compared in rats. Half-lives of the three compounds in rat brain were 3.7, 4.4, and 5.7
    hr, respectively for the 4-fluoro, 4-chloro, and 4-bromo amphetamines. The tendency of the
    drugs to be associated with particulate material in brain homogenates or to prefer an organic
    versus an aqueous phase in uitro varied in the order 4-bromo > 4-chloro > 4-fluoro. This order
    of activity also applied to the inhibition of monoamine oxidase in vitro. All three 4-haloampheta-
    mines reduced the activity of tryptophan hydroxyiase and lowered the levels of serotonin and
    S-hydroxyindoleacetic acid in whole brain initially. With ~chloroamphe~mine and 4-bromoam-
    phetamine, the depletion of brain 5-hydroxyindoies lasted for at least a week. 4-F~uoroampheta-
    mine, in contrast, lowered serotonin and 5-hydroxyindolea~tic acid levels only for short times
    (2-6 hr) after drug injection, and 5-hydroxyindole levels were essentially back to normal within
    24 hr. Prior treatment with an uptake inhibitor prevented the serotonin depletion by all of
    the haloamphetamines, indicating they all required the membrane uptake pump for entry into
    the neurone. The effect of 4-bromoamphetamine, like that of 4-chloroamphetamine, could be
    reversed by subsequent injection of the uptake inhibitor after short periods but not after 2448
    hr. The failure of 4-tluoroamphetamine to produce a long-lasting depletion of brain serotonin
    like that produced by 4chloroamphetamine or 4-bromoamphetamine may reflect the inability of the fluoro-compound to be metabolized in the same way as the other haloamphetamines.