Res Commun Chem Pathol Pharmacol. 1988 Feb;59(2):279-82.
The effect of H2-antagonists on the absorption of bupropion in rats.

al-Khamis KI, Kaka JS, Tanira MO.

Department of Clinical Pharmacy and Research Centre, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

Bupropion absorption was investigated by oral administration of bupropion alone or in combination with cimetidine or ranitidine to rats. Blood samples were collected before and at 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 3.0, 4.5 and 6 h after bupropion administration. The assay of bupropion in plasma was carried out by an HPLC method. Cimetidine or ranitidine did not significantly affect the plasma bupropion concentrations on concurrent administration. No significant differences were observed between area under the curves (AUC)s, maximum plasma concentration, time to peak and the half-life of bupropion among the three groups. These results indicate that neither cimetidine nor ranitidine significantly affects the rate or the extent of bupropion absorption in rats.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2895943&dopt=Abstract Bupropion Wellbutrin




Neuropharmacology. 1986 Dec;25(12):1323-6.
Down regulation of beta-receptors by bupropion and its major metabolite in mouse brain.

Perumal AS, Smith TM, Suckow RF, Cooper TB.

Mice were treated with bupropion Compound II (major metabolite of bupropion) or desmethylimpramine (DMI) twice a day intraperitoneally for either 1 or 3 weeks. The binding of dihydroalprenolol and spiroperidol in the frontal cortex and limbic forebrain areas were analyzed. There was a significant reduction in beta-receptors in the frontal cortex induced by DMI at both times examined. Bupropion showed a significant reduction of beta-receptor in the frontal cortex by 3 weeks. Though propiophenone did not have any significant effect on beta-receptors in the frontal cortex, it down-regulated beta-receptors in the limbic forebrain area significantly by 1 and 3 weeks. There was no significant effect of buropion or propiophenone on the binding of spiroperidol either in the cortex (S2 receptor) or in the limbic forebrain (dopaminergic). These results show that bupropion may exert part of its clinical effect through its metabolite propiophenone.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3031529&dopt=Abstract Bupropion Wellbutrin




Neuropharmacology. 1986 Feb;25(2):199-202.
Effect of plasma from patients containing bupropion and its metabolites on the uptake of norepinephrine.

Perumal AS, Smith TM, Suckow RF, Cooper TB.

The uptake of norepinephrine into cortical punches from the brain of the rat was studied in the presence of buffer and plasma from patients containing bupropion and its metabolites. Even though bupropion and its metabolite (compound II) were equipotent in inhibiting the uptake of NE in buffer, compound II was twice as active as bupropion in the presence of human plasma. When the inhibition of uptake of NE in the presence of plasma, obtained from patients on bupropion on steady-state, was correlated with levels of bupropion and its metabolites (II, III, IV) a highly significant correlation was seen in the presence of compound II. Since this compound accumulated in plasma from patients 20-100 times that of the parent compound, the mode of action of bupropion may in part be due to the effect of this compound on the uptake of NE.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3084990&dopt=Abstract Bupropion Wellbutrin




Pharmacol Biochem Behav. 1986 Apr;24(4):795-9.
Effects of acute and chronic bupropion on locomotor activity and dopaminergic neurons.

Nielsen JA, Shannon NJ, Bero L, Moore KE.

Acute administration of bupropion (10 or 30 mg/kg) to rats increased locomotor activity in a dose-related manner. The highest dose increased the dopamine (DA) concentration while both doses reduced the concentration of dihydroxyphenylacetic acid (DOPAC) in the striatum. The enhancement of locomotor activity and the decrease of striatal DOPAC concentrations were increased with chronic administration (up to 40 days) of bupropion. The rate of DA synthesis in the striatum was increased by the acute administration of d-amphetamine but was not altered by acute or chronic administration of bupropion.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3086903&dopt=Abstract Bupropion Wellbutrin




J Pharm Sci. 1986 Apr;75(4):410-2.
Design and synthesis of a hapten for the radioimmunoassay of bupropion.

Mehta NB, Musso DL.

The synthesis of a hapten useful in the radioimmunoassay of bupropion is described. Since bupropion has no functional group that can be easily derivatized, a hydroxypropyl group was incorporated into the molecule. Studies in cross-reactivity with possible metabolites required the synthesis of the 4'-hydroxy analogue of bupropion. This synthesis is also described.

http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3088255&dopt=Abstract Bupropion Wellbutrin