Document Detail


Effects of fluoxetine and norfluoxetine on 5-hydroxytryptamine metabolism in blood platelets and brain after administration to rats.
MedLine Citation:
PMID:  10052854     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The effects of intraperitoneal administration of fluoxetine (2.5, 5, 10 or 20 mg kg(-1)) and norfluoxetine (10 mg kg(-1)) on 5-hydroxytryptamine (5-HT) and 5-hydroxyindole-3-acetic acid (5-HIAA) metabolism were examined in the blood platelets and brain of rats killed 3 h after a single dose. Several experiments were performed to evaluate the effect of norfluoxetine. Plasma 5-HT concentrations decreased significantly (48%) compared with control group results 3 h after administration of a single dose of fluoxetine (10 or 20 mg kg(-1)). Similar plasma 5-HT levels, 0.54+/-0.04 and 0.56+/-0.09 mg L(-1), respectively, were observed after administration of 10 mg kg(-1) fluoxetine or norfluoxetine. In the same way 5-HIAA levels in whole brain were similar, 0.36+/-0.03 and 0.34+/-0.01 microg(-1), respectively, after administration of fluoxetine or norfluoxetine. There was a good correlation between plasma and brain levels of fluoxetine (0.962) and norfluoxetine (0.957). The results suggest that fluoxetine and norfluoxetine lead to reduced levels of 5-HT in platelets and of 5-HIAA in the brain. Like the parent drug, norfluoxetine is a potent and selective inhibitor of 5-HT uptake.
Authors:
R Bourdeaux; D Desor; P R Lehr; C Younos; B Capolaghi
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Publication Detail:
Type:  Journal Article    
Journal Detail:
Title:  The Journal of pharmacy and pharmacology     Volume:  50     ISSN:  0022-3573     ISO Abbreviation:  J. Pharm. Pharmacol.     Publication Date:  1998 Dec 
Date Detail:
Created Date:  1999-04-29     Completed Date:  1999-04-29     Revised Date:  2003-11-14    
Medline Journal Info:
Nlm Unique ID:  0376363     Medline TA:  J Pharm Pharmacol     Country:  ENGLAND    
Other Details:
Languages:  eng     Pagination:  1387-92     Citation Subset:  IM    
Affiliation:
Laboratoire de Biochimie, CHR Metz-Thionville, Thionville, France.
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MeSH Terms
Descriptor/Qualifier:
Animals
Antidepressive Agents, Second-Generation / pharmacology
Blood Platelets / drug effects*,  metabolism
Brain / drug effects*,  metabolism
Fluoxetine / analogs & derivatives*,  pharmacology*
Hydroxyindoleacetic Acid / blood,  metabolism
Injections, Intraperitoneal
Male
Rats
Rats, Wistar
Serotonin / blood,  metabolism*
Serotonin Uptake Inhibitors / pharmacology*
Chemical
Reg. No./Substance:
0/Antidepressive Agents, Second-Generation; 0/Serotonin Uptake Inhibitors; 50-67-9/Serotonin; 54-16-0/Hydroxyindoleacetic Acid; 54910-89-3/Fluoxetine; 56161-73-0/norfluoxetine

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine


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