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Differences in delta- and mu-opioid receptor blockade measured by positron emission tomography in naltrexone-treated recently abstinent alcohol-dependent subjects
DC Field | Value | Language |
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dc.contributor.author | Weerts, Elise M | - |
dc.contributor.author | Kim, Yu Kyeong | - |
dc.contributor.author | Wand, Gary S | - |
dc.contributor.author | Dannals, Robert F | - |
dc.contributor.author | Lee, Jae Sung | - |
dc.contributor.author | Frost, J James | - |
dc.contributor.author | McCaul, Mary E | - |
dc.date.accessioned | 2010-06-21T23:15:20Z | - |
dc.date.available | 2010-06-21T23:15:20Z | - |
dc.date.issued | 2007-05-10 | - |
dc.identifier.citation | Neuropsychopharmacology 33(3): 653-665 | en |
dc.identifier.issn | 0893-133X (Print) | - |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=17487229 | - |
dc.identifier.uri | http://www.nature.com/npp/journal/v33/n3/pdf/1301440a.pdf | - |
dc.identifier.uri | https://hdl.handle.net/10371/67724 | - |
dc.description.abstract | Blockade of brain mu-opioid receptor (mu-OR) and delta-opioid receptor (delta-OR) was investigated in recently abstinent alcohol-dependent subjects (N=21) maintained on naltrexone. Subjects completed a 19-day inpatient protocol, which included alcohol abstinence followed by naltrexone treatment (50 mg) on days 15-19. Blood samples were collected after the first administration of naltrexone to evaluate serum levels of naltrexone and 6-beta-naltrexol. Regional brain mu-OR binding potential (BP) and delta-OR Ki was measured using [11C]carfentanil (CAR) positron emission tomography (PET) and [11C]methyl naltrindole ([11C]MeNTI) PET, respectively, before (day 5) and during naltrexone treatment (day 18). Naltrexone inhibition of [11C]CAR BP was near maximal across all brain regions of interest with little variability across subjects (mean+SD% inhibition=94.9+4.9%). Naltrexone only partially inhibited the [11C]MeNTI Ki and there was more variability across subjects (mean+SD% inhibition=21.1+14.49%). Peak serum levels of naltrexone were positively correlated with % inhibition of delta-OR Ki in neocortex and basal ganglia. Peak serum levels of naltrexone were not correlated with % inhibition of mu-OR BP. Peak levels of 6-beta-naltrexol were not significantly correlated with % inhibition of mu-OR BP or delta-OR Ki. Thus, the FDA recommended therapeutic dose of naltrexone was sufficient to produce near complete inhibition of the mu-OR in recently abstinent alcohol dependent subjects. The lower percent inhibition of delta-OR and greater variability in delta-OR blockade by naltrexone across subjects may contribute to individual differences in treatment outcomes to naltrexone. Further investigations on the relationship between individual differences in delta-OR blockade by naltrexone and clinical outcomes should be explored. | en |
dc.language.iso | en | en |
dc.publisher | Nature Publishing Group | en |
dc.subject | Adult | en |
dc.subject | Alcoholism/*drug therapy/*radionuclide imaging | en |
dc.subject | Analgesics, Opioid/diagnostic use | en |
dc.subject | Data Interpretation, Statistical | en |
dc.subject | Female | en |
dc.subject | Fentanyl/analogs & derivatives/diagnostic use | en |
dc.subject | Humans | en |
dc.subject | Male | en |
dc.subject | Middle Aged | en |
dc.subject | Naltrexone/blood/pharmacokinetics/*therapeutic use | en |
dc.subject | Narcotic Antagonists/blood/pharmacokinetics/*therapeutic use | en |
dc.subject | Positron-Emission Tomography | en |
dc.subject | Radiopharmaceuticals/diagnostic use | en |
dc.subject | Receptors, Opioid, delta/*antagonists & inhibitors | en |
dc.subject | Receptors, Opioid, mu/*antagonists & inhibitors | en |
dc.subject | Substance Withdrawal Syndrome/psychology/radionuclide imaging | en |
dc.subject | Temperance | en |
dc.title | Differences in delta- and mu-opioid receptor blockade measured by positron emission tomography in naltrexone-treated recently abstinent alcohol-dependent subjects | en |
dc.type | Article | en |
dc.contributor.AlternativeAuthor | 김유경 | - |
dc.contributor.AlternativeAuthor | 이재성 | - |
dc.identifier.doi | 10.1038/sj.npp.1301440 | - |
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