| pubmed-article:3009817 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:3009817 | lifeskim:mentions | umls-concept:C0330390 | lld:lifeskim |
| pubmed-article:3009817 | lifeskim:mentions | umls-concept:C0027410 | lld:lifeskim |
| pubmed-article:3009817 | lifeskim:mentions | umls-concept:C1261322 | lld:lifeskim |
| pubmed-article:3009817 | lifeskim:mentions | umls-concept:C0678594 | lld:lifeskim |
| pubmed-article:3009817 | lifeskim:mentions | umls-concept:C1514873 | lld:lifeskim |
| pubmed-article:3009817 | lifeskim:mentions | umls-concept:C0049408 | lld:lifeskim |
| pubmed-article:3009817 | pubmed:issue | 5 | lld:pubmed |
| pubmed-article:3009817 | pubmed:dateCreated | 1986-6-20 | lld:pubmed |
| pubmed-article:3009817 | pubmed:abstractText | In an effort to determine whether or not the basic nitrogens in the spacer of the bivalent ligand 6 beta,6 beta'-[ethylenebis(oxyethyleneimino)]bis[17-(cyclopropylmethyl)4,5 alpha-epoxymorphinan-3,14-diol] (TENA, 1) is responsible for its selective kappa opioid antagonist activity, we have synthesized monovalent analogues 2-4 that contain a C-6 side chain with basic nitrogens. Analogue 2 behaved as a potent opioid agonist in the guinea pig ileum preparation (GPI) and possessed no significant kappa opioid antagonist activity (IC50 ratio = 1) relative to TENA (IC50 ratio = 20). The agonist activity of 3 and 4 interfered with the opioid antagonist assay and therefore did not permit evaluation of antagonist activity in a concentration range where TENA is effective. Although the results obtained with 2 are consistent with the requirement of a second opiate pharmacophore (rather than a second basic nitrogen in the spacer) for the kappa antagonist activity of TENA, the potent agonism associated with these monomers do not allow a firm conclusion in this regard. | lld:pubmed |
| pubmed-article:3009817 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3009817 | pubmed:language | eng | lld:pubmed |
| pubmed-article:3009817 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3009817 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:3009817 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3009817 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3009817 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3009817 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3009817 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:3009817 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:3009817 | pubmed:month | May | lld:pubmed |
| pubmed-article:3009817 | pubmed:issn | 0022-2623 | lld:pubmed |
| pubmed-article:3009817 | pubmed:author | pubmed-author:PortogheseP... | lld:pubmed |
| pubmed-article:3009817 | pubmed:author | pubmed-author:TakemoriA EAE | lld:pubmed |
| pubmed-article:3009817 | pubmed:author | pubmed-author:BotrosSS | lld:pubmed |
| pubmed-article:3009817 | pubmed:author | pubmed-author:LipkowskiA... | lld:pubmed |
| pubmed-article:3009817 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:3009817 | pubmed:volume | 29 | lld:pubmed |
| pubmed-article:3009817 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:3009817 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:3009817 | pubmed:pagination | 874-6 | lld:pubmed |
| pubmed-article:3009817 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
| pubmed-article:3009817 | pubmed:meshHeading | pubmed-meshheading:3009817-... | lld:pubmed |
| pubmed-article:3009817 | pubmed:meshHeading | pubmed-meshheading:3009817-... | lld:pubmed |
| pubmed-article:3009817 | pubmed:meshHeading | pubmed-meshheading:3009817-... | lld:pubmed |
| pubmed-article:3009817 | pubmed:meshHeading | pubmed-meshheading:3009817-... | lld:pubmed |
| pubmed-article:3009817 | pubmed:meshHeading | pubmed-meshheading:3009817-... | lld:pubmed |
| pubmed-article:3009817 | pubmed:meshHeading | pubmed-meshheading:3009817-... | lld:pubmed |
| pubmed-article:3009817 | pubmed:meshHeading | pubmed-meshheading:3009817-... | lld:pubmed |
| pubmed-article:3009817 | pubmed:meshHeading | pubmed-meshheading:3009817-... | lld:pubmed |
| pubmed-article:3009817 | pubmed:year | 1986 | lld:pubmed |
| pubmed-article:3009817 | pubmed:articleTitle | Investigation of the structural requirements for the kappa-selective opioid receptor antagonist, 6 beta,6 beta'-[ethylenebis(oxyethyleneimino)]bis[17-(cyclopropylmethyl)- 4,5 alpha-epoxymorphinan-3,14-diol] (TENA). | lld:pubmed |
| pubmed-article:3009817 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:3009817 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| http://linkedlifedata.com/r... | http://linkedlifedata.com/r... | pubmed-article:3009817 | lld:chembl |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:3009817 | lld:pubmed |
