Drugs online research references
Psychopharmacology (Berl). 1992;106(2):248-52.
Effects of bupropion on core body temperature of mice.
Zarrindast MR, Abolfathi-Araghi F.
Department of Pharmacology, Medical Faculty, University of Tehran, Iran.
The effects of bupropion on core body temperature of intact or reserpinized mice were studied. Intraperitoneal (IP) administration of bupropion to mice induced a dose-dependent hypothermia. The response of bupropion was decreased by the D-2 antagonist sulpiride or pimozide, but not by the D-1 antagonist SCH 23390, antimuscarinic drug atropine, alpha-adrenergic blocker phenoxybenzimine, beta-adrenergic antagonist propranolol or antiserotonergic methergoline. Reserpine induced hypothermia, which was reversed by bupropion administration. The reversal response of bupropion was reduced by propranolol, but not sulpiride, SCH 23390, phenoxybenzamine, atropine or methergoline. It is concluded that bupropion-induced hypothermia may be mediated through D-2 receptor activation, while the reversal of reserpine-induced hypothermia by bupropion may be exerted through beta-adrenergic stimulation.
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J Clin Psychiatry. 1983 May;44(5 Pt 2):79-81.
Metabolism and kinetics of bupropion.
Schroeder DH.
Studies of bupropion in rats, dogs, and normal volunteers showed that bupropion was rapidly and completely absorbed, widely distributed in tissues, and metabolized extensively prior to its excretion. Metabolism in rats and dogs appeared to be predominantly by side chain oxidative cleavage, while reduction of the intact parent aminoketone to an aminoalcohol was an additional major pathway in man. Most of the metabolites were excreted in urine. Bupropion, but not its metabolites, was concentrated in many tissues, with a brain to plasma ratio of about 25:1. Plasma protein binding of bupropion (75%-80%) did not seem to limit its tissue distribution. Bupropion was found to be a weak to moderate inducer of drug metabolism.
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Neuropsychopharmacology. 1992 Aug;7(1):7-14.
Effects of chronic bupropion on interstitial concentrations of dopamine in rat nucleus accumbens and striatum.
Nomikos GG, Damsma G, Wenkstern D, Fibiger HC.
Department of Psychiatry, University of British Columbia, Vancouver, Canada.
Bupropion is a novel atypical antidepressant that inhibits dopamine (DA) uptake. The present experiments investigated the effects of acute (10 mg/kg, twice daily for 2 days) and chronic (10 mg/kg, twice daily for 21 days) bupropion treatment on interstitial DA concentrations using simultaneous in vivo microdialysis in the nucleus accumbens (NAC) and striatum of awake freely moving rats. Compared to animals that had not previously been exposed to the drug, bupropion (25 mg/kg, IP) induced increases in extracellular DA were significantly enhanced in the NAC of the chronic but not the acute bupropion group. This effect was regionally selective, as it was not observed in the striatum. In accordance with previous reports, concurrent behavioral measurements indicated that the locomotor stimulant effects of bupropion were also enhanced in the chronic group. These results demonstrate that bupropion-induced behavioral sensitization is accompanied by a selective potentiation of the effects of this compound on interstitial DA concentrations in the NAC.
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