| pubmed-article:12887410 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:12887410 | lifeskim:mentions | umls-concept:C0243192 | lld:lifeskim |
| pubmed-article:12887410 | lifeskim:mentions | umls-concept:C0066908 | lld:lifeskim |
| pubmed-article:12887410 | lifeskim:mentions | umls-concept:C1521970 | lld:lifeskim |
| pubmed-article:12887410 | lifeskim:mentions | umls-concept:C1167622 | lld:lifeskim |
| pubmed-article:12887410 | lifeskim:mentions | umls-concept:C1510827 | lld:lifeskim |
| pubmed-article:12887410 | lifeskim:mentions | umls-concept:C0659802 | lld:lifeskim |
| pubmed-article:12887410 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:12887410 | pubmed:dateCreated | 2003-7-30 | lld:pubmed |
| pubmed-article:12887410 | pubmed:abstractText | The highly potent micro -opioid receptor agonist 14-methoxymetopon (4,5alpha-epoxy-3-hydroxy-14beta-methoxy-5beta,17-dimethylmorphinan-6-one) was prepared in tritium labelled form by a catalytic dehalogenation method resulting in a specific radioactivity of 15.9 Ci/mmol. Opioid binding characteristics of [3H]14-methoxymetopon were determined using radioligand binding assay in rat brain membranes. [3H]14-Methoxymetopon specifically labelled a single class of opioid sites with affinity in low subnanomolar range (Ki = 0.43 nm) and maximal number of binding sites of 314 fmol/mg protein. Binding of [3H]14-methoxymetopon was inhibited by ligands selective for the micro -opioid receptor with high potency, while selective kappa-opioids and delta-opioids were weaker inhibitors. 14-Methoxymetopon increased guanosine-5'-O-(3-[35S]thio)-triphosphate ([35S]GTPgammaS) binding with an EC50 of 70.9 nm, thus, providing evidence for the agonist character of this ligand. The increase of [35S]GTPgammaS binding was inhibited by naloxone and selective micro -opioid antagonists, indicating a micro -opioid receptor-mediated action. [3H]14-Methoxymetopon is one of the few nonpeptide mu-opioid receptor agonists available in radiolabelled form up to now. Due to its high affinity and selectivity, high stability and extremely low nonspecific binding (<10%), this radioligand would be an important and useful tool in probing mu-opioid receptor mechanisms, as well as to promote a further understanding of the opioid system at the cellular and molecular level. | lld:pubmed |
| pubmed-article:12887410 | pubmed:language | eng | lld:pubmed |
| pubmed-article:12887410 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12887410 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:12887410 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12887410 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12887410 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12887410 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12887410 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12887410 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:12887410 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:12887410 | pubmed:month | Jul | lld:pubmed |
| pubmed-article:12887410 | pubmed:issn | 0953-816X | lld:pubmed |
| pubmed-article:12887410 | pubmed:author | pubmed-author:OtvösFerencF | lld:pubmed |
| pubmed-article:12887410 | pubmed:author | pubmed-author:SpeteaMariana... | lld:pubmed |
| pubmed-article:12887410 | pubmed:author | pubmed-author:SchmidhammerH... | lld:pubmed |
| pubmed-article:12887410 | pubmed:author | pubmed-author:BorsodiAnnaA | lld:pubmed |
| pubmed-article:12887410 | pubmed:author | pubmed-author:TóthGézaG | lld:pubmed |
| pubmed-article:12887410 | pubmed:author | pubmed-author:SchützJohanne... | lld:pubmed |
| pubmed-article:12887410 | pubmed:author | pubmed-author:TóthFanniF | lld:pubmed |
| pubmed-article:12887410 | pubmed:author | pubmed-author:BenyheSandorS | lld:pubmed |
| pubmed-article:12887410 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:12887410 | pubmed:volume | 18 | lld:pubmed |
| pubmed-article:12887410 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:12887410 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:12887410 | pubmed:pagination | 290-5 | lld:pubmed |
| pubmed-article:12887410 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:meshHeading | pubmed-meshheading:12887410... | lld:pubmed |
| pubmed-article:12887410 | pubmed:year | 2003 | lld:pubmed |
| pubmed-article:12887410 | pubmed:articleTitle | Binding characteristics of [3H]14-methoxymetopon, a high affinity mu-opioid receptor agonist. | lld:pubmed |
| pubmed-article:12887410 | pubmed:affiliation | Division of Pharmaceutical Chemistry, Department of Pharmacy, University of Innsbruck, Innrain 52a, A-6020 Innsbruck, Austria. Mariana.Spetea@uibk.ac.at | lld:pubmed |
| pubmed-article:12887410 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:12887410 | pubmed:publicationType | Research Support, Non-U.S. Gov't | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:12887410 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:12887410 | lld:pubmed |
