Source:http://linkedlifedata.com/resource/pubmed/id/18762712
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
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pubmed:dateCreated |
2008-9-2
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pubmed:abstractText |
We have recently identified a Na+/Cl--coupled transport system in mammalian cells for endogenous and synthetic opioid peptides. This transport system does not transport dipeptides/tripeptides, but is stimulated by these small peptides. Here we investigated the influence of L-kyotorphin (L-Tyr-L-Arg), an endogenous dipeptide with opioid activity, on this transport system. The activity of the transport system, measured in SK-N-SH cells (a human neuronal cell line) with deltorphin II as a model substrate, was stimulated approximately 2.5-fold by L-kyotorphin, with half-maximal stimulation occurring at approximately 100 microM. The stimulation was associated primarily with an increase in the affinity for deltorphin II. The stimulation caused by L-kyotorphin was stereospecific; L-Tyr-D-Arg (D-kyotorphin) had minimal effect. The influence of L-kyotorphin was observed also in a different cell line which expressed the opioid peptide transport system. While L-kyotorphin is a stimulator of opioid peptide transport, it is a transportable substrate for the H+-coupled peptide transporter PEPT2, which is expressed widely in the brain. Since the activity of the opioid peptide transport system is modulated by extracellular L-kyotorphin and since PEPT2 is an important determinant of extracellular L-kyotorphin in the brain, the expression/activity of PEPT2 may be a critical factor in the modulation of opioidergic neurotransmission in vivo.
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pubmed:grant | |
pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Chlorides,
http://linkedlifedata.com/resource/pubmed/chemical/Endorphins,
http://linkedlifedata.com/resource/pubmed/chemical/Oligopeptides,
http://linkedlifedata.com/resource/pubmed/chemical/Opioid Peptides,
http://linkedlifedata.com/resource/pubmed/chemical/Sodium,
http://linkedlifedata.com/resource/pubmed/chemical/Symporters,
http://linkedlifedata.com/resource/pubmed/chemical/deltorphin II, Ala(2)-,
http://linkedlifedata.com/resource/pubmed/chemical/glycyl-glycyl-phenylalaninamide,
http://linkedlifedata.com/resource/pubmed/chemical/hydrogen-coupled oligopeptide...,
http://linkedlifedata.com/resource/pubmed/chemical/kyotorphin
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pubmed:status |
MEDLINE
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pubmed:issn |
1880-0920
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:volume |
23
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
254-62
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pubmed:meshHeading |
pubmed-meshheading:18762712-Animals,
pubmed-meshheading:18762712-Biological Transport,
pubmed-meshheading:18762712-Cell Line,
pubmed-meshheading:18762712-Chlorides,
pubmed-meshheading:18762712-Dose-Response Relationship, Drug,
pubmed-meshheading:18762712-Endorphins,
pubmed-meshheading:18762712-Humans,
pubmed-meshheading:18762712-Oligopeptides,
pubmed-meshheading:18762712-Opioid Peptides,
pubmed-meshheading:18762712-Sodium,
pubmed-meshheading:18762712-Stereoisomerism,
pubmed-meshheading:18762712-Symporters,
pubmed-meshheading:18762712-Xenopus laevis
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pubmed:year |
2008
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pubmed:articleTitle |
Stimulation of Na+/Cl--coupled opioid peptide transport system in SK-N-SH cells by L-kyotorphin, an endogenous substrate for H+-coupled peptide transporter PEPT2.
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pubmed:affiliation |
Department of Biochemistry and Molecular Biology, Medical College of Georgia, Augusta, GA 30912, USA.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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