| pubmed-article:8749027 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:8749027 | lifeskim:mentions | umls-concept:C0026549 | lld:lifeskim |
| pubmed-article:8749027 | lifeskim:mentions | umls-concept:C0597357 | lld:lifeskim |
| pubmed-article:8749027 | lifeskim:mentions | umls-concept:C0035696 | lld:lifeskim |
| pubmed-article:8749027 | lifeskim:mentions | umls-concept:C0066908 | lld:lifeskim |
| pubmed-article:8749027 | lifeskim:mentions | umls-concept:C1280500 | lld:lifeskim |
| pubmed-article:8749027 | lifeskim:mentions | umls-concept:C0597358 | lld:lifeskim |
| pubmed-article:8749027 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:8749027 | lifeskim:mentions | umls-concept:C0172521 | lld:lifeskim |
| pubmed-article:8749027 | pubmed:issue | 2 | lld:pubmed |
| pubmed-article:8749027 | pubmed:dateCreated | 1996-10-24 | lld:pubmed |
| pubmed-article:8749027 | pubmed:abstractText | In these experiments, the effect of the irreversible mu-opioid receptor antagonist clocinnamox on the potency of morphine, opioid receptor binding and mu-opioid receptor mRNA was examined. Mice were injected with clocinnamox (0.32-12.8 mg/kg) and the analgesic potency of morphine was examined 24 h later. Clocinnamox produced a dose-dependent decrease in the potency of morphine; and at the higher dose of clocinnamox the maximal analgesic effect was not observed following doses of morphine in excess of 500 mg/kg s.c. In saturation binding studies in brain, clocinnamox (0.32-25.6 mg/kg) dose-dependently decreased mu-opioid ([3H][D-Ala2,MePhe4,Gly-ol5]enkephalin; DAMGO) receptor Bmax with relatively minimal effects on Kd. Binding to delta-opioid receptor ([3H][D-Pen2,D-Pen5]enkephalin; DPDPE) and kappa-opioid receptor ([3H](5,7,8)-(-)-N-methyl-N-(7-(1-pyrrolidinyl)-1-oxaspiro(4,5)dec -8-yl) benzeneacetamide; U69,593) was not affected by clocinnamox. The effect of clocinnamox was time-dependent in that the greatest changes in morphine potency and mu-opioid receptor density were observed within 24 h of administration and decreased with time (336 h). Although mu-opioid receptor density was decreased to less than 30% of control 24 h following clocinnamox (12.8 mg/kg) and had increased to 80% by 5 days, a solution hybridization assay for mu-opioid receptor mRNA transcript revealed no changes in the steady-state levels of this mRNA. These studies indicate that clocinnamox is an irreversible antagonist at the mu-opioid receptor since it appears to selectively affect receptor density with minimal effects on affinity. Furthermore, clocinnamox produces time- and dose-dependent changes in Bmax and these changes appear to be unrelated to changes in mu-opioid receptor mRNA. It is possible that the repopulation of brain by mu-opioid receptors following clocinnamox is mediated by an existing pool of receptors that are activated following treatment. | lld:pubmed |
| pubmed-article:8749027 | pubmed:language | eng | lld:pubmed |
| pubmed-article:8749027 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8749027 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:8749027 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8749027 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8749027 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8749027 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8749027 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8749027 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8749027 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:8749027 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:8749027 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:8749027 | pubmed:issn | 0014-2999 | lld:pubmed |
| pubmed-article:8749027 | pubmed:author | pubmed-author:InturrisiC... | lld:pubmed |
| pubmed-article:8749027 | pubmed:author | pubmed-author:ChaoJJ | lld:pubmed |
| pubmed-article:8749027 | pubmed:author | pubmed-author:BrodskyMM | lld:pubmed |
| pubmed-article:8749027 | pubmed:author | pubmed-author:FranklinSS | lld:pubmed |
| pubmed-article:8749027 | pubmed:author | pubmed-author:DavisTT | lld:pubmed |
| pubmed-article:8749027 | pubmed:author | pubmed-author:YoburnB CBC | lld:pubmed |
| pubmed-article:8749027 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:8749027 | pubmed:day | 12 | lld:pubmed |
| pubmed-article:8749027 | pubmed:volume | 287 | lld:pubmed |
| pubmed-article:8749027 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:8749027 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:8749027 | pubmed:pagination | 135-43 | lld:pubmed |
| pubmed-article:8749027 | pubmed:dateRevised | 2006-11-15 | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:meshHeading | pubmed-meshheading:8749027-... | lld:pubmed |
| pubmed-article:8749027 | pubmed:year | 1995 | lld:pubmed |
| pubmed-article:8749027 | pubmed:articleTitle | The effect of the irreversible mu-opioid receptor antagonist clocinnamox on morphine potency, receptor binding and receptor mRNA. | lld:pubmed |
| pubmed-article:8749027 | pubmed:affiliation | Department of Pharmaceutical Sciences, College of Pharmacy and Allied Health Professions, St. John's University, Queens, NY 11439, USA. | lld:pubmed |
| pubmed-article:8749027 | pubmed:publicationType | Journal Article | lld:pubmed |
| pubmed-article:8749027 | pubmed:publicationType | Research Support, U.S. Gov't, P.H.S. | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:8749027 | lld:pubmed |
| http://linkedlifedata.com/r... | pubmed:referesTo | pubmed-article:8749027 | lld:pubmed |
