Effects of Mg-pemoline on the central catecholaminergic system.
Acute or repeated treatment with Mg-Pemoline (Mg-Pg) did not modify the endogenous level of brain catecholamines (CA) of rats. However, a single dose (30 mg/kg) produced a significant decrease of brain CA turnover, measured either by the rate of conversion of 14C-tyrosine to CA or by the rate of disappearance of CA after alpha-MT. Mg-Pe (0.01-0.1 mM) did not modify the basal outflow nor the release of 3H-DA elicited by high K+ in slices of corpus striatum. At the same concentrations, Mg-Pe inhibited uptake of DA (competitively) or NA (uncompetitively) in synaptosomes from corpus striatum and hypothalamus, respectively. Turning-behavior in mice lesioned in corpus striatum with 6-OH-DA, indicated that this drug acts like amphetamine as an indirect DA agonist. These results suggest that central stimulant effects of Mg-Pe may be the consequence of CA-uptake inhibition and this effect may also account for the decrease of brain CA turnover.
D000818:Animals; D001923:Brain Chemistry / Q000187:drug effects*; D002395:Catecholamines / Q000502:physiology*; D003342:Corpus Striatum / Q000378:metabolism; D006801:Humans; D007031:Hypothalamus / Q000378:metabolism; D007700:Kinetics; D008297:Male; D010389:Pemoline / Q000494:pharmacology*; D051381:Rats; D011954:Receptors, Dopamine / Q000187:drug effects; D013045:Species Specificity; D013239:Stereotyped Behavior / Q000187:drug effects; D013574:Synaptosomes / Q000378:metabolism
D002395:Catecholamines; D011954:Receptors, Dopamine; D010389:Pemoline