Drugs online research references
Neuropharmacology. 2000 Aug 23;39(11):1974-83.
Amplification of cortical serotonin release: a further neurochemical action of the vigilance-promoting drug modafinil.
Ferraro L, Fuxe K, Tanganelli S, Fernandez M, Rambert FA, Antonelli T.
Department of Experimental and Clinical Medicine, Section of Pharmacology, University of Ferrara, Ferrara, Italy.
The present in vitro and in vivo studies examined the effects of modafinil on serotonergic transmission in the rat frontal cortex. In the in vitro study modafinil (0.3-30 microM) increased electrically-evoked, but not spontaneous, serotonin ([(3)H]5-HT) efflux from cortical slices in a concentration-dependent manner while the indirect serotonin agonist dl-fenfluramine (1-15 microM) enhanced both spontaneous and evoked [(3)H]5-HT efflux. The effects of modafinil were more pronounced when the 5-HT reuptake was blocked by paroxetine. Contrary to paroxetine (0.3-3 microM) and dl-fenfluramine (1-5 microM), modafinil failed to influence the [(3)H]5-HT uptake. In the in vivo study modafinil (3-100 mg/kg i.p.) increased 5-HT dialysate levels, the maximal effect being already reached at the 30 mg/kg dose. dl-fenfluramine (5 mg/kg) induced an increase in 5-HT levels which was significantly higher than that displayed by modafinil at 30 mg/kg. In the presence of paroxetine (3 microM), the effect of modafinil at 30 mg/kg was higher than that observed in the absence of 5-HT reuptake inhibition. Finally, in the presence of the selective 5-HT(1A) receptor agonist 8-OH-DPAT, modafinil at 100 mg/kg failed to affect 5-HT dialysate levels.These results demonstrate that modafinil regulates cortical serotonergic transmission and suggest that the drug preferentially acts by amplifying the electro-neurosecretory coupling mechanisms and via mechanisms which do not involve the reuptake process.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10963741&dopt=Abstract
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The effect of sibutramine and dexfenfluramine on 5-HT re-uptake sites, labelled with [(3)H]paroxetine, have been determined in various rat brain regions. In addition, the ability of fluoxetine and sibutramine to protect against the changes in [(3)H]paroxetine binding produced by dexfenfluramine was examined. Sibutramine (9 mg/kg, p.o.) and dexfenfluramine (1, 3 and 10 mg/kg, p.o.) were administered twice daily (before 09.00 h and after 16.00 h) for four days, followed by a 14 day drug-free period. In the protection studies, fluoxetine (10 mg/kg, i.p.) and sibutramine (9 mg/kg, p.o.) were given 1 h prior to dexfenfluramine (10 mg/kg, p.o.) using the same dosing regimen as described above. Sibutramine (9 mg/kg, p.o.; three times its ED(50) to inhibit food intake at 2 h) had no significant effect on the number or affinity of 5-HT re-uptake sites the brain regions studied. In contrast, dexfenfluramine at an equivalent dose (3 mg/kg, p.o.) significantly decreased the number of 5-HT re-uptake sites in frontal cortex (by 35%), hippocampus (by 47%) and hypothalamus (by 27%). This effect was dose-dependent with marked decreases (by 58-84%) in the number of sites following 10 mg/kg, p.o. These effects were not associated with changes in binding affinity. Fluoxetine (10 mg/kg, i.p.) completely blocked the effect of dexfenfluramine (10 mg/kg, p.o.) without having any significant effect alone. Sibutramine (9 mg/kg, p.o.) also blocked the effects of dexfenfluramine, although the reversal was only partial in frontal cortex, hippocampus and hypothalamus. Thus sibutramine, unlike dexfenfluramine, does not alter brain 5-HT re-uptake sites. Furthermore, sibutramine and fluoxetine protect against the deficits in 5-HT re-uptake sites produced by dexfenfluramine. These data provide further evidence that sibutramine is a 5-HT re-uptake inhibitor and it does not have neurotoxic potential.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10963746&dopt=Abstract
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Eur J Pharmacol. 2000 Sep 1;403(1-2):55-65.
Effects of acute and chronic tianeptine administration on serotonin outflow in rats: comparison with paroxetine by using in vivo microdialysis.
Malagie I, Deslandes A, Gardier AM.
Laboratoire de Neuropharmacologie, UPRES EAD MENRT, Faculte de Pharmacie IFR-ISIT, Institut de Signalisation et Innovation Therapeutique, Universite Paris-Sud, F92296 Chatenay-Malabry, France.
Using in vivo microdialysis, we compared the effects of tianeptine (an antidepressant drug which, in marked contrast with other antidepressants, is thought to increase the uptake of serotonin (5-hydroxytryptamine, 5-HT) on extracellular 5-HT concentrations ([5-HT](ext)) in the frontal cortex and raphe nuclei of freely moving rats with those of paroxetine, a potent selective serotonin reuptake inhibitor. A single paroxetine dose (1 mg/kg, i.p.) increased [5-HT](ext) over baseline in the frontal cortex and raphe nuclei, respectively. A single administration of tianeptine (10 mg/kg, i.p.) did not change [5-HT(ext)] in the two brain regions studied. Repeated exposure to paroxetine (0.5 mg/kg) b.i.d. for 14 days induced a sixfold significant increase in basal [5-HT](ext) in the raphe nuclei. Administration of tianeptine (5 mg/kg) b.i.d. for 14 days did not affect 5-HT baseline concentrations. In rats chronically treated with either paroxetine or tianeptine, drug challenge did not alter area under the curve values. Thus, our in vivo data indicate that tianeptine and paroxetine do not exert a similar in vivo effect on the serotonergic system in rat brain.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=10969144&dopt=Abstract
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