| pubmed-article:2893264 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:2893264 | lifeskim:mentions | umls-concept:C0034801 | lld:lifeskim |
| pubmed-article:2893264 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:2893264 | pubmed:dateCreated | 1988-3-18 | lld:pubmed |
| pubmed-article:2893264 | pubmed:abstractText | H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) exhibited high affinity (IC50 = 2.80 nM) in displacing [3H]naloxone binding (nH = 0.89 +/- 0.1) and showed an exceptional selectivity for mu opioid receptors with an IC50(DPDPE)/IC50(naloxone) ratio of 4,840, while it displayed very low affinity for somatostatin receptors (IC50 = 22,700 nM) in rat brain binding assays. [3H]CTOP was recently custom synthesized (spec. act.: 84 Ci/mmol) and evaluated for its in vitro binding properties towards the mu opioid receptors in rat brain membrane preparations. Association and dissociation of [3H]CTOP binding to mu opioid receptors were rapid at 25 degrees C with a kinetic Kd value of 0.67 nM. Saturation experiments gave apparent Kd value of 1.11 nM and Bmax value of 136 +/- 13 fmol/mg prot at 25 degrees C. Specific [3H]CTOP binding was inhibited by a number of different opioid and opiate ligands. Among them, putative mu opioid receptor-specific ligands, such as naloxone, naltrexone and CTOP inhibited the binding with high affinity, while delta opioid receptor-specific compounds or non-opioid drugs inhibited specific [3H]CTOP binding with low affinity or they were ineffective. | lld:pubmed |
| pubmed-article:2893264 | pubmed:language | eng | lld:pubmed |
| pubmed-article:2893264 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:2893264 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:2893264 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:2893264 | pubmed:issn | 1046-9516 | lld:pubmed |
| pubmed-article:2893264 | pubmed:author | pubmed-author:YamamuraH IHI | lld:pubmed |
| pubmed-article:2893264 | pubmed:author | pubmed-author:HrubyV JVJ | lld:pubmed |
| pubmed-article:2893264 | pubmed:author | pubmed-author:PeltonJ TJT | lld:pubmed |
| pubmed-article:2893264 | pubmed:author | pubmed-author:LuiG KGK | lld:pubmed |
| pubmed-article:2893264 | pubmed:author | pubmed-author:GulyaKK | lld:pubmed |
| pubmed-article:2893264 | pubmed:author | pubmed-author:KazmierskiWW | lld:pubmed |
| pubmed-article:2893264 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:2893264 | pubmed:volume | 75 | lld:pubmed |
| pubmed-article:2893264 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:2893264 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:2893264 | pubmed:pagination | 209-12 | lld:pubmed |
| pubmed-article:2893264 | pubmed:dateRevised | 2003-11-14 | lld:pubmed |
| pubmed-article:2893264 | pubmed:meshHeading | pubmed-meshheading:2893264-... | lld:pubmed |
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| pubmed-article:2893264 | pubmed:year | 1986 | lld:pubmed |
| pubmed-article:2893264 | pubmed:articleTitle | H-D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2: a potent and selective antagonist opioid receptors. | lld:pubmed |
| pubmed-article:2893264 | pubmed:affiliation | Department of Pharmacology, University of Arizona, Tucson 85724. | lld:pubmed |
| pubmed-article:2893264 | pubmed:publicationType | Journal Article | lld:pubmed |
