Resolution of Biphasic Binding of the Opioid Antagonist Naltrexone in Brain Membranes
dc.contributor.author | Remraers, Ann E. | en_US |
dc.contributor.author | Medzihradsky, Fedor | en_US |
dc.date.accessioned | 2010-04-01T15:50:43Z | |
dc.date.available | 2010-04-01T15:50:43Z | |
dc.date.issued | 1991-10 | en_US |
dc.identifier.citation | Remraers, Ann E.; Medzihradsky, Fedor (1991). "Resolution of Biphasic Binding of the Opioid Antagonist Naltrexone in Brain Membranes." Journal of Neurochemistry 57(4): 1265-1269. <http://hdl.handle.net/2027.42/66340> | en_US |
dc.identifier.issn | 0022-3042 | en_US |
dc.identifier.issn | 1471-4159 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/66340 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=1654389&dopt=citation | en_US |
dc.description.abstract | In synaptosomal membranes from rat brain cortex, in the presence of 150 m M NaC1, the opioid antagonist [ 3 H] naltrexone bound to two populations of receptor sites with affinities of 0.27 and 4.3 n M , respectively. Guanosine-5′-(3-thiotriphosphate) had little modulating effect and did not alter the biphasic nature of ligand binding. On the other hand, receptor-selective opioids differentially inhibited the two binding components of [ 3 H] naltrexone. As shown by nonlinear least-squares analysis, the Μ opioids Tyr-D-Ala-Gly-(Me)Phe-Gly-ol or sufentanil abolished high-affinity [ 3 H] naltrexone binding, whereas the Δ-selective ligands [D- Pen 2 , D-Pen 5 ] enkephalin, ICI 174, 864, and oxymorphindole inhibited and eventually eliminated the low-affinity component in a concentration-dependent manner. These results indicate that, in contrast to the guanine nucleotide-sensitive biphasic binding of opioid-alkaloid agonists, the heterogeneity of naltrexone binding in brain membranes reflects ligand interaction with different opioid-receptor types. | en_US |
dc.format.extent | 493355 bytes | |
dc.format.extent | 3110 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.publisher | Blackwell Publishing Ltd | en_US |
dc.rights | 1991 International Society for Neurochemistry | en_US |
dc.subject.other | Opioid Receptors | en_US |
dc.subject.other | Agonist-antagonist Binding | en_US |
dc.subject.other | Μ- and Δ-Se- Lective Opioids | en_US |
dc.subject.other | [ 3 H] Naltrexone | en_US |
dc.subject.other | Rat Brain Cortex | en_US |
dc.title | Resolution of Biphasic Binding of the Opioid Antagonist Naltrexone in Brain Membranes | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Neurosciences | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Departments of Biological Chemistry and Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, U.S.A. | en_US |
dc.identifier.pmid | 1654389 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/66340/1/j.1471-4159.1991.tb08288.x.pdf | |
dc.identifier.doi | 10.1111/j.1471-4159.1991.tb08288.x | en_US |
dc.identifier.source | Journal of Neurochemistry | en_US |
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dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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