Detail of "64609-06-9"

Reference

Comparison between the neurotoxic and serotonin-depleting effects of various halogenated derivatives of amphetamine in the rat

Comparison between the neurotoxic and serotonin-depleting effects of various halogenated derivatives of amphetamine in the rat. Harvey, John A.; McMaster, Scott E.; Fuller, Ray W. (Dep. Psychol., Univ. Iowa, Iowa City, Iowa, USA). J. Pharmacol. Exp. Ther., 202(3), 581-9 (English) 1977. CODEN: JPETAB. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) In rats dosages of 100 .mu.mol/kg of 4-chloroamphetamine-HCl (I) [3706-38-5], 4-bromoamphetamine-HCl [64609-05-8] or fenfluramine [458-24-2] produced marked evidence of a neurotoxic reaction restricted primarily to cells in the B-9 region. The reacting cells displayed an intense staining of Nissl substance or intense deposition of silver throughout the cell body, a shrunken and abnormal shape and a perineuronal space. This intense cytophathol. reaction was correlated with significant decreases in brain content of serotonin [50-67-9]. Both the neurotoxic action and depletion of brain serotonin produced by I and fenfluramine were completely blocked by pretreatment with fluoxetine, an inhibitor of serotonin uptake. 4-Fluoroamphetamine-HCl [64609-06-9] (100 .mu.mol/kg) and .beta.,.beta.-difluoro-4-chloroamphetamine-HCl [64609-07-0] (400 .mu.mol/kg) were devoid of any neurotoxic action and failed to produce a long-term (3-day) depletion of serotonin. Thus at least part of the long-term decrease in serotonin previously obsd. to occur after I, 4-bromoamphetamine, and fenfluramine might be due to their entry into, and irreversible destruction of, B-9 serotonergic cell bodies.

Inhibition of cell-free protein synthesis initiation by amphetamine: association with reduction in tRNA aminoacylation

Inhibition of cell-free protein synthesis initiation by amphetamine: association with reduction in tRNA aminoacylation. Nowak, Thaddeus S.; Munro, Hamish N. (Dep. Nutr. Food Sci., Massachusetts Inst. Technol., Cambridge, Mass., USA). Biochem. Biophys. Res. Commun., 77(4), 1280-5 (English) 1977. CODEN: BBRCA9. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) In homologous initiating and non-initiating protein synthesis systems prepd. from rabbit reticulocytes, 4-10 mM D-amphetamine sulfate [51-63-8] preferentially inhibited initiation-dependent amino acid incorporation without affecting elongation, in agreement with previous results using wheat germ initiating and rat elongating systems. A test of several para-substituted amphetamines yielded an order of potency: DL-p-hydroxyamphetamine-HBr [140-36-3] < DL-p-fluoroamphetamine-HCl [64609-06-9] .simeq. amphetamine < DL-p-chloroamphetamine-HCl [3706-38-5] < DL-p-bromoamphetamine-HCl [64609-05-8]. Over the same concn. range at which these compds. inhibited protein synthesis, they proportionately inhibited aminoacylation of tRNA, suggesting that this may be responsible for their inhibitory action on protein synthesis.