| pubmed-article:2872570 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:2872570 | lifeskim:mentions | umls-concept:C0037659 | lld:lifeskim |
| pubmed-article:2872570 | lifeskim:mentions | umls-concept:C0066908 | lld:lifeskim |
| pubmed-article:2872570 | lifeskim:mentions | umls-concept:C1510827 | lld:lifeskim |
| pubmed-article:2872570 | lifeskim:mentions | umls-concept:C0243071 | lld:lifeskim |
| pubmed-article:2872570 | pubmed:issue | 24 | lld:pubmed |
| pubmed-article:2872570 | pubmed:dateCreated | 1986-7-23 | lld:pubmed |
| pubmed-article:2872570 | pubmed:abstractText | A series of cyclic conformationally restricted penicillamine containing somatostatin octapeptide analogues have been prepared by standard solid phase synthetic techniques and tested for their ability to inhibit specific [125I]CGP 23,996 (des-Ala1-,Gly2-[desamino-Cys3Tyr11]-dicarba3, 14-somatostatin), [3H]naloxone or [3H]DPDPE ([D-Pen2-D-Pen5]enkephalin) binding in rat brain membrane preparations. We now report structure-activity relationship studies with the synthesis of our most potent and selective mu opioid receptor compound D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2, which we refer to as Cys2Tyr3Orn5Pen7-amide. While this octapeptide exhibited high affinity (IC50 = 2.80 nM) for an apparently single population of binding sites (nH = 0.89 +/- 0.1) and exceptional selectivity for mu opioid receptors with an IC50(DPDPE)/IC50 (naloxone) ratio of 4,829, it also displayed very low affinity for somatostatin receptors (IC50 = 22,700 nM). Thus, Cys2Tyr3Orn5Pen7-amide may be the ligand of choice for further characterization of mu opioid receptors and for examining the physiological role of this class of receptors. | lld:pubmed |
| pubmed-article:2872570 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:grant | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:language | eng | lld:pubmed |
| pubmed-article:2872570 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2872570 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:2872570 | pubmed:month | Jun | lld:pubmed |
| pubmed-article:2872570 | pubmed:issn | 0024-3205 | lld:pubmed |
| pubmed-article:2872570 | pubmed:author | pubmed-author:YamamuraH IHI | lld:pubmed |
| pubmed-article:2872570 | pubmed:author | pubmed-author:HrubyV JVJ | lld:pubmed |
| pubmed-article:2872570 | pubmed:author | pubmed-author:PeltonJ TJT | lld:pubmed |
| pubmed-article:2872570 | pubmed:author | pubmed-author:GulyaKK | lld:pubmed |
| pubmed-article:2872570 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:2872570 | pubmed:day | 16 | lld:pubmed |
| pubmed-article:2872570 | pubmed:volume | 38 | lld:pubmed |
| pubmed-article:2872570 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:2872570 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:2872570 | pubmed:pagination | 2221-9 | lld:pubmed |
| pubmed-article:2872570 | pubmed:dateRevised | 2007-11-14 | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:meshHeading | pubmed-meshheading:2872570-... | lld:pubmed |
| pubmed-article:2872570 | pubmed:year | 1986 | lld:pubmed |
| pubmed-article:2872570 | pubmed:articleTitle | Cyclic somatostatin octapeptide analogues with high affinity and selectivity toward mu opioid receptors. | lld:pubmed |
| pubmed-article:2872570 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:2872570 | pubmed:publicationType | Comparative Study | lld:pubmed |
| pubmed-article:2872570 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:2872570 | lld:pubmed |
