| pubmed-article:15860577 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:15860577 | lifeskim:mentions | umls-concept:C0020792 | lld:lifeskim |
| pubmed-article:15860577 | lifeskim:mentions | umls-concept:C0005496 | lld:lifeskim |
| pubmed-article:15860577 | lifeskim:mentions | umls-concept:C0170657 | lld:lifeskim |
| pubmed-article:15860577 | lifeskim:mentions | umls-concept:C0596902 | lld:lifeskim |
| pubmed-article:15860577 | lifeskim:mentions | umls-concept:C2603343 | lld:lifeskim |
| pubmed-article:15860577 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:15860577 | lifeskim:mentions | umls-concept:C0031957 | lld:lifeskim |
| pubmed-article:15860577 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:15860577 | pubmed:dateCreated | 2005-7-18 | lld:pubmed |
| pubmed-article:15860577 | pubmed:abstractText | Previous studies identified partial inhibitors of serotonin (5-HT) transporter and dopamine transporter binding. We report here on a partial inhibitor of 5-HT transporter (SERT) binding identified among a group of 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine analogs (4-[2-[bis(4-fluorophenyl)-methoxy]ethyl]-1-(2-trifluoromethyl-benzyl)-piperidine; TB-1-099). Membranes were prepared from rat brains or human embryonic kidney cells expressing the cloned human dopamine (hDAT), serotonin (hSERT), and norepinephrine (hNET) transporters. beta-(4'-(125)Iodophenyl)tropan-2beta-carboxylic acid methyl ester ([(125)I]RTI-55) binding and other assays followed published procedures. Using rat brain membranes, TB-1-099 weakly inhibited DAT binding (K(i) = 439 nM), was inactive at NET binding ([(3)H]nisoxetine), and partially inhibited SERT binding with an extrapolated plateau ("A" value) of 20%. Similarly, TB-1-099 partially inhibited [(125)I]RTI-55 binding to hSERT with an extrapolated plateau (A value) of 14%. Upon examining the effect of increasing concentrations of TB-1-099 on the apparent K(d) and B(max) of [(125)I]RTI-55 binding to hSERT, we found that TB-1-099 decreased the B(max) in a dose-dependent manner and affected the apparent K(d) in a manner well described by a sigmoid dose-response curve. TB-1-099 increased the K(d) but not to the magnitude expected for a competitive inhibitor. In rat brain synaptosomes, TB-1-099 noncompetitively inhibited [(3)H]5-HT, but not [(3)H]dopamine, uptake. Dissociation experiments indicated that TB-1-099 promoted the rapid dissociation of a small component of [(125)I]RTI-55 binding to hSERT. Association experiments demonstrated that TB-1-099 slowed [(125)I]RTI-55 binding to hSERT in a manner unlike that of the competitive inhibitor indatraline. Viewed collectively, these results support the hypothesis that TB-1-099 allosterically modulates hSERT binding and function. | lld:pubmed |
| pubmed-article:15860577 | pubmed:language | eng | lld:pubmed |
| pubmed-article:15860577 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15860577 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:15860577 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:15860577 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15860577 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:15860577 | pubmed:month | Aug | lld:pubmed |
| pubmed-article:15860577 | pubmed:issn | 0022-3565 | lld:pubmed |
| pubmed-article:15860577 | pubmed:author | pubmed-author:JacobsonArthu... | lld:pubmed |
| pubmed-article:15860577 | pubmed:author | pubmed-author:RiceKenner... | lld:pubmed |
| pubmed-article:15860577 | pubmed:author | pubmed-author:DerschChristi... | lld:pubmed |
| pubmed-article:15860577 | pubmed:author | pubmed-author:RothmanRichar... | lld:pubmed |
| pubmed-article:15860577 | pubmed:author | pubmed-author:CalhounWillia... | lld:pubmed |
| pubmed-article:15860577 | pubmed:author | pubmed-author:NightingaleBa... | lld:pubmed |
| pubmed-article:15860577 | pubmed:author | pubmed-author:GreinerElisab... | lld:pubmed |
| pubmed-article:15860577 | pubmed:author | pubmed-author:BoosTerrence... | lld:pubmed |
| pubmed-article:15860577 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:15860577 | pubmed:volume | 314 | lld:pubmed |
| pubmed-article:15860577 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:15860577 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:15860577 | pubmed:pagination | 906-15 | lld:pubmed |
| pubmed-article:15860577 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
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| pubmed-article:15860577 | pubmed:year | 2005 | lld:pubmed |
| pubmed-article:15860577 | pubmed:articleTitle | Studies of the biogenic amine transporters. XI. Identification of a 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR12909) analog that allosterically modulates the serotonin transporter. | lld:pubmed |
| pubmed-article:15860577 | pubmed:affiliation | Clinical Psychopharmacology Section, Intramural Research Program, National Institute on Drug Abuse, National Institutes of Health, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA. | lld:pubmed |
| pubmed-article:15860577 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:15860577 | pubmed:publicationType | In Vitro | lld:pubmed |
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