Linked Life Data

14566196

Source:http://linkedlifedata.com/resource/pubmed/id/14566196

Statements in which the resource exists as a subject.
PredicateObject
rdf:type
lifeskim:mentions
pubmed:dateCreated
2003-10-20
pubmed:abstractText
Paroxetine is a potent and selective serotonin reuptake inhibitor (SSRI) with some neuropharmacologic properties unique among this class of compounds. The findings of early in vitro studies demonstrated the potency of paroxetine at inhibiting 5-HT uptake in rat synaptosomes. Paroxetine also has been shown to be a potent and selective inhibitor of the human serotonin transporter (SERT) and has recently been demonstrated to have moderate affinity for the norepinephrine transporter (NET). Because of the affinity and in vitro selectivity of this SSRI, tritiated paroxetine is now widely used as a marker for SERT in laboratory settings, and its use has advanced our understanding of neurotransmitter function in the brain and periphery. The in vivo pharmacologic properties of paroxetine are well characterized, especially following acute administration. However, the pharmacologic effects of chronically administered paroxetine remain an active area of study. Paroxetine administration in laboratory animals has been shown to be associated with decreased SERT density and function, maintenance of normal firing rates and release of 5-HT, and increased activation of postsynaptic 5-HT receptors. Using a novel ex vivo assay, we have demonstrated that paroxetine exhibits dose-related inhibition of the NET in patients treated for depression. At usual clinical doses (ie, 20 mg/d), paroxetine is a potent and selective inhibitor of the SERT; however, at higher doses (ie, 40 mg/d), paroxetine can exhibit marked NET inhibition. The application of these findings of in vivo NET inhibition by paroxetine in the treatment of mood and anxiety disorders will be informed by further clinical studies.
pubmed:language
eng
pubmed:journal
pubmed:citationSubset
IM
pubmed:chemical
http://linkedlifedata.com/resource/pubmed/chemical/Antidepressive Agents..., http://linkedlifedata.com/resource/pubmed/chemical/Carrier Proteins, http://linkedlifedata.com/resource/pubmed/chemical/Membrane Glycoproteins, http://linkedlifedata.com/resource/pubmed/chemical/Membrane Transport Proteins, http://linkedlifedata.com/resource/pubmed/chemical/Nerve Tissue Proteins, http://linkedlifedata.com/resource/pubmed/chemical/Norepinephrine Plasma Membrane..., http://linkedlifedata.com/resource/pubmed/chemical/Paroxetine, http://linkedlifedata.com/resource/pubmed/chemical/SLC6A2 protein, human, http://linkedlifedata.com/resource/pubmed/chemical/SLC6A4 protein, human, http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Plasma Membrane..., http://linkedlifedata.com/resource/pubmed/chemical/Serotonin Uptake Inhibitors, http://linkedlifedata.com/resource/pubmed/chemical/Symporters
pubmed:status
MEDLINE
pubmed:issn
0048-5764
pubmed:author
pubmed:issnType
Print
pubmed:volume
37 Suppl 1
pubmed:owner
NLM
pubmed:authorsComplete
Y
pubmed:pagination
8-18
pubmed:dateRevised
2009-11-11
pubmed:meshHeading
pubmed:year
2003
pubmed:articleTitle
Neuropharmacology of paroxetine.
pubmed:affiliation
Department of Psychiatry and Behavioral Sciences, Emory University School of Medicine, Atlanta, Georgia 30322, USA. mowens@emory.edu
pubmed:publicationType
Journal Article, Review, Research Support, Non-U.S. Gov't