Receptor binding, antagonist, and withdrawal precipitating properties of opiate antagonists
dc.contributor.author | Valentino, Rita J. | en_US |
dc.contributor.author | Katz, Jonathan L. | en_US |
dc.contributor.author | Medzihradsky, Fedor | en_US |
dc.contributor.author | Woods, James H. | en_US |
dc.date.accessioned | 2006-04-07T18:41:08Z | |
dc.date.available | 2006-04-07T18:41:08Z | |
dc.date.issued | 1983-06-20 | en_US |
dc.identifier.citation | Valentino, Rita J., Katz, Jonathan L., Medzihradsky, Fedor, Woods, James H. (1983/06/20)."Receptor binding, antagonist, and withdrawal precipitating properties of opiate antagonists." Life Sciences 32(25): 2887-2896. <http://hdl.handle.net/2027.42/25182> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6T99-478B6T2-2HR/2/5ebaf18b9293c6c32ca78a370737932c | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/25182 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=6304445&dopt=citation | en_US |
dc.description.abstract | A number of opiate antagonists and the dextro isomers of some of these drugs were studied for antagonism of acute opiate effects on ilea isolated from opiate-naive guinea pigs, precipitation of a withdrawal contraction of ilea isolated from morphine-dependent guinea pigs, precipitation of withdrawal in morphine-dependent rhesus monkeys and stereospecific displacement of 3H-etorphine binding to rat-brain membranes. With the exception of -naloxone, all of the compounds displaced 3H-etorphine. With the exception of -naloxone, nalorphine, and quaternary nalorphine, all of the antagonists caused a contraction of ilea isolated from morphine-dependent guinea pigs. Moreover, the IC 50 values of the compounds for displacing 3H-etorphine binding were well correlated with both their Ke values for antagonism in the ileum (r = 0.95) and with their EC 50 values for precipitating a contraction in this preparation (r = 0.92). Generally, the concentration of antagonist necessary to precipitate half maximal contracture was 30-fold greater than the Ke value of the antagonist. Most of the opiate antagonists also precipitated withdrawal when administered to morphine-dependent rhesus monkeys and their potencies were well correlated with their potencies in ileum (with Ke: r = 0.95; with EC 50: r = 0.99) and in displacing 3H-etorphine (r = 0.95). The quaternary derivative of naltrexone, however, was an effective opiate antagonist only , and was ineffective in precipitating withdrawal in morphine-dependent rhesus monkeys. These results suggest that the receptor sites labeled by 3H-etorphine are the same as those involved in antagonism of acute opiate actions and in precipitation of withdrawal. | en_US |
dc.format.extent | 654963 bytes | |
dc.format.extent | 3118 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Elsevier | en_US |
dc.title | Receptor binding, antagonist, and withdrawal precipitating properties of opiate antagonists | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Natural Resources and Environment | en_US |
dc.subject.hlbsecondlevel | Molecular, Cellular and Developmental Biology | en_US |
dc.subject.hlbsecondlevel | Ecology and Evolutionary Biology | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.subject.hlbtoplevel | Science | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | Department of Pharmacology, The University of Michigan Medical School, Ann Arbor, MI 48109, USA | en_US |
dc.contributor.affiliationum | Department of Pharmacology, The University of Michigan Medical School, Ann Arbor, MI 48109, USA | en_US |
dc.contributor.affiliationum | Department of Pharmacology, The University of Michigan Medical School, Ann Arbor, MI 48109, USA; Department of Biological Chemistry, The University of Michigan Medical School, Ann Arbor, MI 48109, USA | en_US |
dc.contributor.affiliationum | Department of Pharmacology, The University of Michigan Medical School, Ann Arbor, MI 48109, USA; Department of Psychology, The University of Michigan Medical School, Ann Arbor, MI 48109, USA | en_US |
dc.identifier.pmid | 6304445 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/25182/1/0000621.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0024-3205(83)90325-9 | en_US |
dc.identifier.source | Life Sciences | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
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