| pubmed-article:16321540 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:16321540 | lifeskim:mentions | umls-concept:C0382336 | lld:lifeskim |
| pubmed-article:16321540 | lifeskim:mentions | umls-concept:C0034801 | lld:lifeskim |
| pubmed-article:16321540 | lifeskim:mentions | umls-concept:C0558295 | lld:lifeskim |
| pubmed-article:16321540 | lifeskim:mentions | umls-concept:C1417964 | lld:lifeskim |
| pubmed-article:16321540 | lifeskim:mentions | umls-concept:C1709915 | lld:lifeskim |
| pubmed-article:16321540 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:16321540 | lifeskim:mentions | umls-concept:C0772162 | lld:lifeskim |
| pubmed-article:16321540 | lifeskim:mentions | umls-concept:C0086191 | lld:lifeskim |
| pubmed-article:16321540 | pubmed:issue | 7 | lld:pubmed |
| pubmed-article:16321540 | pubmed:dateCreated | 2006-2-21 | lld:pubmed |
| pubmed-article:16321540 | pubmed:abstractText | Nociceptin (NOC) and dynorphin A (DYN) analogues containing 2',6'-dimethylphenylalanine (Dmp) in place of Phe or Tyr in position 1 and/or 4 were synthesized and their metabolic stability and receptor-binding properties were investigated. [Dmp1]NOC(1-13)-NH2 (1) possessed high ORL1 receptor affinity comparable to that of the parent peptide with substantially improved affinities for kappa-, mu-, and delta-opioid receptors. However, Dmp4 substitution of NOC peptide (2) reduced ORL1 receptor affinity. [Dmp1]DYN(1-13)-NH2 (4) and its Dmp4 analogue (5) possessed a 3-fold greater kappa-opioid receptor affinity and improved kappa-receptor selectivity compared to the parent peptide. Analogue 4 however exhibited an unexpectedly low in vitro bioactivity (GPI assay), suggesting, the phenolic hydroxyl group at the N-terminal residue in DYN peptide is extremely important for activation of the kappa-opioid receptor. Analogue 5 possessed an improved kappa-opioid receptor selectivity with an IC50 ratio of 1(kappa)/509(mu)/211598(delta); thus, this peptide may serve as a highly selective kappa-receptor agonist for pharmacological study. Dmp1 substitution in both the NOC and DYN peptides improved metabolic stability toward these peptides, while Dmp4 substitution provided no additional metabolic stability. | lld:pubmed |
| pubmed-article:16321540 | pubmed:language | eng | lld:pubmed |
| pubmed-article:16321540 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:16321540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:16321540 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:16321540 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:16321540 | pubmed:issn | 0968-0896 | lld:pubmed |
| pubmed-article:16321540 | pubmed:author | pubmed-author:AmboAkihiroA | lld:pubmed |
| pubmed-article:16321540 | pubmed:author | pubmed-author:SasakiYusukeY | lld:pubmed |
| pubmed-article:16321540 | pubmed:author | pubmed-author:KoharaHirokaz... | lld:pubmed |
| pubmed-article:16321540 | pubmed:author | pubmed-author:KawanoSusumuS | lld:pubmed |
| pubmed-article:16321540 | pubmed:author | pubmed-author:WatanabeHidek... | lld:pubmed |
| pubmed-article:16321540 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:16321540 | pubmed:day | 1 | lld:pubmed |
| pubmed-article:16321540 | pubmed:volume | 14 | lld:pubmed |
| pubmed-article:16321540 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:16321540 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:16321540 | pubmed:pagination | 2433-7 | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:meshHeading | pubmed-meshheading:16321540... | lld:pubmed |
| pubmed-article:16321540 | pubmed:year | 2006 | lld:pubmed |
| pubmed-article:16321540 | pubmed:articleTitle | ORL1 and opioid receptor preferences of nociceptin and dynorphin A analogues with Dmp substituted for N-terminal aromatic residues. | lld:pubmed |
| pubmed-article:16321540 | pubmed:affiliation | Tohoku Pharmaceutical University, 4-1 Komatsushima 4-chome, Aoba-ku, Sendai 981-8558, Japan. ysasaki@tohoku-pharm.ac.jp | lld:pubmed |
| pubmed-article:16321540 | pubmed:publicationType | Journal Article | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:16321540 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:16321540 | lld:pubmed |
