Estimation of the affinity of naloxone at supraspinal and spinal opioid receptors in vivo: Studies with receptor selective agonists
dc.contributor.author | Heyman, Julius S. | en_US |
dc.contributor.author | Koslo, Randy J. | en_US |
dc.contributor.author | Mosberg, Henry I. | en_US |
dc.contributor.author | Tallarida, Ronald J. | en_US |
dc.contributor.author | Porreca, Frank | en_US |
dc.date.accessioned | 2006-04-07T19:24:13Z | |
dc.date.available | 2006-04-07T19:24:13Z | |
dc.date.issued | 1986-11-10 | en_US |
dc.identifier.citation | Heyman, Julius S., Koslo, Randy J., Mosberg, Henry I., Tallarida, Ronald J., Porreca, Frank (1986/11/10)."Estimation of the affinity of naloxone at supraspinal and spinal opioid receptors in vivo: Studies with receptor selective agonists." Life Sciences 39(19): 1795-1803. <http://hdl.handle.net/2027.42/25982> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6T99-4751TBJ-2JH/2/9732654134fcdb9f633ab177ff30d948 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/25982 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=3022095&dopt=citation | en_US |
dc.description.abstract | The apparent affinity of naloxone at cerebral and spinal sites was estimated using selective mu [D-Ala2, Gly-ol5]-enkephalin (DAGO) and delta [D-Pen2, D-Pen5]enkephalin] (DPDPE) opioid agonists in the mouse warm water tail-withdrawal test in vivo; the mu agonist morphine was employed as a reference compound. The approach was to determine the naloxone pA2 using a time-dependent method with both agonist and antagonist given intracerebroventricularly (i.c.v.) or intrathecally (i.th.); naloxone was always given 5 min before the agonist. Complete time-response curves were determined for each agonist at each site in the absence, and in the presence, of a single, fixed i.c.v. or i.th. dose of naloxone. From these i.c.v. or i.th. pairs of time-response curves, pairs of dose-response lines were constructed at various times; these lines showed decreasing displacement with time, indicative of the disappearance of naloxone. The graph of log (dose ratio - 1) vs. time was linear with negative slope, in agreement with the time-dependent form of the equation for competitive antagonism. From this plot, the apparent pA2 and naloxone half-life was calculated at each site and against each agonist. The affinity of naloxone was not significantly different when compared between agonists after i.c.v. administration. A small difference was seen between the affinity of i.th. naloxone against DPDPE and DAGO; the i.th. naloxone pA2 against morphine, however, was not different than that for DPDPE and DAGO. The naloxone half-life varied between 6.6 and 16.9 min, values close to those previously reported for this compound. These results suggest that the agonists studied may produce their i.c.v. analgesic effects at the same receptor type or that alternatively, the naloxone pA2 may be fortuitously similar for mu and delta receptors in vivo. Additionally, while the affinity of naloxone appears different for the receptors activated by i.th. DAGO and DPDPE, further work may be necessary before firm conclusions regarding the nature of the spinal analgesic receptor(s) can be drawn. | en_US |
dc.format.extent | 538223 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 | Estimation of the affinity of naloxone at supraspinal and spinal opioid receptors in vivo: Studies with receptor selective agonists | 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 | College of Pharmacy, University of Michigan, Ann Arbor, MI 48109, USA | en_US |
dc.contributor.affiliationother | Bristol-Myers Products, Hillside, NJ 07207, USA | en_US |
dc.contributor.affiliationother | Bristol-Myers Products, Hillside, NJ 07207, USA | en_US |
dc.contributor.affiliationother | Department of Pharmacology, Temple University Medical School, Philadelphia, PA 19102, USA | en_US |
dc.contributor.affiliationother | Department of Pharmacology, University of Arizona Health Sciences Center, Tucson, AZ 85724, USA | en_US |
dc.identifier.pmid | 3022095 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/25982/1/0000048.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0024-3205(86)90099-8 | en_US |
dc.identifier.source | Life Sciences | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
Files in this item
Remediation of Harmful Language
The University of Michigan Library aims to describe library materials in a way that respects the people and communities who create, use, and are represented in our collections. Report harmful or offensive language in catalog records, finding aids, or elsewhere in our collections anonymously through our metadata feedback form. More information at Remediation of Harmful Language.
Accessibility
If you are unable to use this file in its current format, please select the Contact Us link and we can modify it to make it more accessible to you.