Comparison of 4-chloro-, 4-bromo- and 4-fluoroamphetamine in rats: Drug levels in brain and effects on brain serotonin metabolism

  title={Comparison of 4-chloro-, 4-bromo- and 4-fluoroamphetamine in rats: Drug levels in brain and effects on brain serotonin metabolism},
  author={Ray W. Fuller and John C. Baker and Kenneth W. Perry and Bryan B. Molloy},

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p-Chloroamphetamine (PCA), 3,4-methylenedioxymethamphetamine (MDMA) andd-fenfluramine pretreatment attenuatesd-fenfluramine-evoked release of 5-HT in vivo
The present data are consistent with the hypothesis that the acute release of 5-HT evoked by d-fenfluramine occurs via those terminals destroyed by pretreatment with PCA, MDMA andd-fen fluramine, while KCl evokes release from bothPCA-sensitive and PCA-insensitive terminals.
  • J. Harvey
  • Biology, Chemistry
    Annals of the New York Academy of Sciences
  • 1978
Some of the anatomic evidence that has been obtained concerning the neurotoxic effects of various halogenated amphetamines by the use of Nissland silver-stained sections of brain are described.
A First-in-Man Study with 4-Fluoroamphetamine Demonstrates it Produces a Mild Psychedelic State
It is concluded that while the 4- FA-induced psychedelic state is mild in intensity and in between that produced by amphetamine and MDMA as hypothesized, more research is needed to indicate whether 4-FA can change creative thinking.


Effect of , -difluoro substitution on the disposition and pharmacological effects of 4-chloroamphetamine in rats.
The results suggest the difluoro compound is metabolized more rapidly and to a greater extent in rats than is 4-chloroamphetamine, and the physiologic disposition and pharmacologic effects of the drug are markedly altered.
Effects of some homologues of 4-chloroamphetamine on brain serotonin metabolism.
Effect of four amphetamines on brain biogenic amines and their metabolites.
  • B. Leonard
  • Biology, Chemistry
    Biochemical pharmacology
  • 1972
Long-term effects of 4-chloroamphetamine on brain 5-hydroxyindole metabolism in rats.
Reversible and irreversible phases of serotonin depletion by 4-chloroamphetamine.
Studies on sympathomimetic amines. II. The biotransformation and physiological disposition of d-amphetamine, d-p-hydroxyamphetamine and d-methamphetamine.
  • J. Axelrod
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1954
d-Amphetamine disappears slowly in the dog compared to its hydroxylated derivative, suggesting that in this species the major part of the pharmacological effect of the drug is due to the parent compound.
Tissue levels of chloroamphetamines in rats and mice.
During the first 4 hr. after i.p. injection of equimolar amounts of the two drugs, more 4-chloroamphetamine than amphetamine was present in the brain and other tissues of rats and mice, which may be due to blocking of a major metabolic pathway for amphetamine by the para substitution.