Drugs online research references









Psychopharmacology (Berl). 1992;107(2-3):303-9.
A comparison of the effects of sibutramine hydrochloride, bupropion and methamphetamine on dopaminergic function: evidence that dopamine is not a pharmacological target for sibutramine.

Heal DJ, Frankland AT, Gosden J, Hutchins LJ, Prow MR, Luscombe GP, Buckett WR.

Boots Pharmaceuticals Research Department, Nottingham, UK.

Sibutramine hydrochloride, a novel monoamine reuptake inhibitor antidepressant, has been studied to determine whether it alters dopaminergic function in the brain. Its effects have been compared with bupropion, a dopamine reuptake inhibitor, and methamphetamine, a dopamine reuptake inhibitor and releasing agent. Sibutramine (0.1-3 mg/kg PO) and methamphetamine (0.3-30 mg/kg PO) both prevented reserpine (0.75 mg/kg IV) ptosis in rats with ED50 values of 0.6 mg/kg and 4.2 mg/kg, respectively. Bupropion (10-100 mg/kg PO) was ineffective against reserpine ptosis. The efflux of [3H]-dopamine from preloaded rat striatal slices was not altered by 10(-7)-10(-5) M concentrations of sibutramine, BTS 54,354, BTS 54,505 (secondary and primary amine metabolites, respectively) or bupropion. In contrast, methamphetamine (10(-8)-10(-4) M) caused a significant concentration-dependent increase in [3H]-dopamine release. Sibutramine (3 mg/kg IP or 6 mg/kg PO) and bupropion (10 mg/kg IP or 30 mg/kg PO) did not alter 3-methoxytyramine (3-MT) levels in rat striatum. Striatal 3-MT concentrations were, however, dose-dependently increased by methamphetamine (0.3-10 mg/kg IP or 0.42-4.2 mg/kg PO). Sibutramine (6 mg/kg PO) did not induce circling in rats with unilateral 6-hydroxydopamine lesions of the nigrostriatal dopaminergic neuronal tract. Bupropion (10-100 mg/kg PO) did not induce circling at the lowest dose, but caused increasing ipsilateral rotation at higher doses. Methamphetamine (0.42 or 4.2 mg/kg PO) induced ipsilateral circling with marked effects at the higher dose.(ABSTRACT TRUNCATED AT 250 WORDS)

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=1615130&dopt=Abstract

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Biull Eksp Biol Med. 1990 Dec;110(12):616-7.
[Specifics of participation of dopaminergic and serotoninergic systems of the brain in latent inhibition based on pharmacological models]

[Article in Russian]

Loskutova LV, Luk'ianenko FIa.

Single intraperitoneal injections of haloperidol (0.5 mg/kg) or sertralin (5 mg/kg) or 20 preexpositions of conditional stimulus before conditioning induced similar changes of passive avoidance reactions of rats. The combinative application of drugs (sertralin 1h and bupropion 30 min before conditioning) simultaneously enhancing activity of serotonin and dopamine in brain did not produce changes of passive avoidance reaction comparing with intact control. The results obtained showed that high selective drugs and analysis of latent inhibition of some parameters enable creation of pharmacological models and their use as instrument at experimental study of neurochemical mechanisms of attention.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2128040&dopt=Abstract

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Neuropharmacology. 1989 Dec;28(12):1383-8.
Dissociation of the actions of uptake blockers upon dopamine overflow and uptake in the rat nucleus accumbens: in vivo voltammetric data.

Stamford JA, Kruk ZL, Millar J.

Department of Pharmacology, London Hospital Medical College, U.K.

Fast cyclic voltammetry, at carbon fibre microelectrodes, was used to monitor stimulated overflow and uptake of DA in the nucleus accumbens of the rat. Several recognised blockers of neuronal uptake of DA were examined for their actions on each process. Benztropine, cocaine, GBR 12909 and nomifensine elevated the overflow of DA, while only nomifensine and bupropion blocked uptake. The actions of the drugs upon uptake did not correlate with their effects on overflow of DA. It is therefore concluded that the mechanisms by which the drugs influence overflow and uptake are different. It cannot be assumed that the elevation of extracellular DA is solely the result of blockade of uptake by these drugs.

online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2533329&dopt=Abstract

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