| pubmed-article:17339114 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:17339114 | lifeskim:mentions | umls-concept:C0242402 | lld:lifeskim |
| pubmed-article:17339114 | lifeskim:mentions | umls-concept:C0024337 | lld:lifeskim |
| pubmed-article:17339114 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
| pubmed-article:17339114 | lifeskim:mentions | umls-concept:C2603343 | lld:lifeskim |
| pubmed-article:17339114 | lifeskim:mentions | umls-concept:C0599740 | lld:lifeskim |
| pubmed-article:17339114 | lifeskim:mentions | umls-concept:C1120262 | lld:lifeskim |
| pubmed-article:17339114 | pubmed:issue | 9 | lld:pubmed |
| pubmed-article:17339114 | pubmed:dateCreated | 2007-4-2 | lld:pubmed |
| pubmed-article:17339114 | pubmed:abstractText | A wide range of activities are induced by Lys when introduced at C-terminus of the delta-opioid Dmt-Tic pharmacophore through the alpha-amine group, including: improved delta-antagonism, mu-agonism and mu-antagonism. Here we report the synthesis of a new series of compounds with the general formula H-Dmt-Tic-NH-(CH(2))(4)-CH(R)-R' (R=-NH(2), -NH-Ac, -NH-Z; R'=CO-NH-Ph, -CO-NH-CH(2)-Ph, -Bid) in which Lys is linked to Dmt-Tic through its side-chain amine group. All new compounds (1-9) displayed potent and selective delta-antagonism (MVD, pA(2)=7.81-8.27), which was independent of the functionalized alpha-amine and carboxylic groups of C-terminal Lys. This behaviour suggests a direct application as a prototype intermediate, such as Boc-Dmt-Tic-epsilon-Lys(Z)-OMe, which could be successfully applied in the synthesis (after Z or methyl ester removal) of unique designed multiple ligands containing the pharmacophore of the quintessential delta-antagonist Dmt-Tic and another opioid or biologically active non-opioid ligand. | lld:pubmed |
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| pubmed-article:17339114 | pubmed:language | eng | lld:pubmed |
| pubmed-article:17339114 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:17339114 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:17339114 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
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| pubmed-article:17339114 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:17339114 | pubmed:month | May | lld:pubmed |
| pubmed-article:17339114 | pubmed:issn | 0968-0896 | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:BalboniGianfr... | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:SalvadoriSeve... | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:BryantSharon... | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:LazarusLawren... | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:CongiuCenzoC | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:OnnisValentin... | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:AmboAkihiroA | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:SasakiYusukeY | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:JinsmaaYunden... | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:TrapellaClaud... | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:ZottiMargheri... | lld:pubmed |
| pubmed-article:17339114 | pubmed:author | pubmed-author:LazzariIlaria... | lld:pubmed |
| pubmed-article:17339114 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:17339114 | pubmed:day | 1 | lld:pubmed |
| pubmed-article:17339114 | pubmed:volume | 15 | lld:pubmed |
| pubmed-article:17339114 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:17339114 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:17339114 | pubmed:pagination | 3143-51 | lld:pubmed |
| pubmed-article:17339114 | pubmed:dateRevised | 2011-9-19 | lld:pubmed |
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| pubmed-article:17339114 | pubmed:meshHeading | pubmed-meshheading:17339114... | lld:pubmed |
| pubmed-article:17339114 | pubmed:meshHeading | pubmed-meshheading:17339114... | lld:pubmed |
| pubmed-article:17339114 | pubmed:meshHeading | pubmed-meshheading:17339114... | lld:pubmed |
| pubmed-article:17339114 | pubmed:meshHeading | pubmed-meshheading:17339114... | lld:pubmed |
| pubmed-article:17339114 | pubmed:meshHeading | pubmed-meshheading:17339114... | lld:pubmed |
| pubmed-article:17339114 | pubmed:meshHeading | pubmed-meshheading:17339114... | lld:pubmed |
| pubmed-article:17339114 | pubmed:year | 2007 | lld:pubmed |
| pubmed-article:17339114 | pubmed:articleTitle | Further studies on the effect of lysine at the C-terminus of the Dmt-Tic opioid pharmacophore. | lld:pubmed |
| pubmed-article:17339114 | pubmed:affiliation | Department of Toxicology, University of Cagliari, I-09124 Cagliari, Italy. gbalboni@unica.it <gbalboni@unica.it> | lld:pubmed |
| pubmed-article:17339114 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:17339114 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| pubmed-article:17339114 | pubmed:publicationType | Research Support, N.I.H., Intramural | lld:pubmed |
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