| pubmed-article:19256502 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:19256502 | lifeskim:mentions | umls-concept:C0036751 | lld:lifeskim |
| pubmed-article:19256502 | lifeskim:mentions | umls-concept:C0070829 | lld:lifeskim |
| pubmed-article:19256502 | lifeskim:mentions | umls-concept:C0599702 | lld:lifeskim |
| pubmed-article:19256502 | lifeskim:mentions | umls-concept:C0243077 | lld:lifeskim |
| pubmed-article:19256502 | lifeskim:mentions | umls-concept:C1554184 | lld:lifeskim |
| pubmed-article:19256502 | pubmed:issue | 6 | lld:pubmed |
| pubmed-article:19256502 | pubmed:dateCreated | 2009-3-19 | lld:pubmed |
| pubmed-article:19256502 | pubmed:abstractText | A new class of multitarget compounds was synthesized by linking a novel selective serotonin reuptake inhibitor (SSRI) to a PDE4 inhibitor. The new dual PDE4 inhibitor/SSRI showed antidepressant-like activity in the forced swim test in mice The SSRIs 2-{5-[3-(5-fluoro-2-methoxy-phenyl)-ethyl]-tetrahydro-furan-2-yl}-ethylamine (14) and 2-{5-[3-(5-fluoro-2-methoxy-phenyl)-propyl]-tetrahydro-furan-2-yl}-ethylamine (15) were both individually linked to the PDE4 inhibitor 4-(3,4-dimethoxy-phenyl)-4a,5,8,8a-tetrahydro-2H-phthalazin-1-one (19), via a five-carbon chain. The dual PDE4 inhibitor/SSRI 2-{5-[3-(5-fluoro-2-methoxy-phenyl)-ethyl]-tetrahydro-furan-2-yl}-ethylamine)-pentyl]-4,5,8,8a-tetrahydro-2H-phthalazin-1-one (21) showed potent and selective serotonin reuptake inhibition (IC(50) value of 127 nM). The dual PDE4 inhibitor/SSRI 21 also inhibited PDE4D3 with a K(i) value of 2.0 nM. The dual PDE4 inhibitor/SSRI was significantly more effective than the individual SSRI alone or fluoxetine in the forced swim test at standard doses. On a molar basis, the antidepressant-like effect of the dual PDE4 inhibitor/SSRI 21 showed a 129-fold increase in in vivo efficacy compared to fluoxetine. | lld:pubmed |
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| pubmed-article:19256502 | pubmed:language | eng | lld:pubmed |
| pubmed-article:19256502 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19256502 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:19256502 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19256502 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19256502 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:19256502 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:19256502 | pubmed:month | Mar | lld:pubmed |
| pubmed-article:19256502 | pubmed:issn | 1520-4804 | lld:pubmed |
| pubmed-article:19256502 | pubmed:author | pubmed-author:O'DonnellJame... | lld:pubmed |
| pubmed-article:19256502 | pubmed:author | pubmed-author:CashmanJohn... | lld:pubmed |
| pubmed-article:19256502 | pubmed:author | pubmed-author:ZhangHan-Ting... | lld:pubmed |
| pubmed-article:19256502 | pubmed:author | pubmed-author:VoelkerTroyT | lld:pubmed |
| pubmed-article:19256502 | pubmed:issnType | Electronic | lld:pubmed |
| pubmed-article:19256502 | pubmed:day | 26 | lld:pubmed |
| pubmed-article:19256502 | pubmed:volume | 52 | lld:pubmed |
| pubmed-article:19256502 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:19256502 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:19256502 | pubmed:pagination | 1530-9 | lld:pubmed |
| pubmed-article:19256502 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:meshHeading | pubmed-meshheading:19256502... | lld:pubmed |
| pubmed-article:19256502 | pubmed:year | 2009 | lld:pubmed |
| pubmed-article:19256502 | pubmed:articleTitle | Dual inhibitors of phosphodiesterase-4 and serotonin reuptake. | lld:pubmed |
| pubmed-article:19256502 | pubmed:affiliation | Human BioMolecular Research Institute, 5310 Eastgate Mall, San Diego, California 92121, USA. jcashman@hbri.org | lld:pubmed |
| pubmed-article:19256502 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:19256502 | pubmed:publicationType | Research Support, N.I.H., Extramural | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:19256502 | lld:chembl |
