Coupling of multiple opioid receptors to GTPase following selective receptor alkylation in brain membranes
dc.contributor.author | Clark, Mary J. | en_US |
dc.contributor.author | Medzihradsky, Fedor | en_US |
dc.date.accessioned | 2006-04-07T19:45:39Z | |
dc.date.available | 2006-04-07T19:45:39Z | |
dc.date.issued | 1987-12 | en_US |
dc.identifier.citation | Clark, Mary J., Medzihradsky, F. (1987/12)."Coupling of multiple opioid receptors to GTPase following selective receptor alkylation in brain membranes." Neuropharmacology 26(12): 1763-1770. <http://hdl.handle.net/2027.42/26499> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6T0C-478NHFD-KK/2/c980e5064411db4205ccdbe17029e0bc | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/26499 | |
dc.identifier.uri | http://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=2830555&dopt=citation | en_US |
dc.description.abstract | Opioid agonists of the mu, kappa and delta types stimulated low-Km guanosine triphosphatase (GTPase) in membranes, from the brain of the rat by up to 34%, with potencies the rank order of which corresponded to the respective binding affinities to opioid receptor. In general, kappa ligands stimulated GTPase to a lesser degree than mu or delta opiates. The coupling of a given type of opioid receptor to GTPase was resolved by direct or protective alkylation of the other receptors. Treatment of the membranes with [beta]-funaltrexamine abolished the stimulation of GTPase by sufentanil and levorphanol (mu), but not by bremazocine (kappa) or DSLET (delta). On the other hand, prior incubation with Superfit, an alkylating agent with selectivity for the delta opioid receptor, specifically eliminated the effect of DSLET. Partial alkylation by increasing concentrations of Superfit gradually reduced the extent of stimulation of GTPase by DSLET. The successive treatment of membranes with Superfit and [beta]-funaltrex-amine blocked the actions of DSLET, sufentanil and levorphanol, but had no effect on the stimulation of the GTPase by bremazocine. Selective coupling of an opioid receptor to GTPase was also obtained after incubation of membranes with [beta]-chlornaltrexamine in the presence of protective concentrations of mu, kappa or delta opioid ligands. Alkylation resolved the coupling of the non-selective opiate etorphine: the sum of stimulation of GTPase in the receptor-selective membranes equalled maximal stimulation of enzyme in untreated membranes. Naloxone blocked the stimulation of GTPase by mu, kappa or delta agonists, but ICI-174,864 specifically inhibited the effect of DSLET. The results describe the use of receptor-selective membranes from brain to characterize the coupling of multiple opioid receptors to high-affinity GTPase, the inhibitory binding protein for GTP of the adenylate cyclase complex. | en_US |
dc.format.extent | 974622 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 | Coupling of multiple opioid receptors to GTPase following selective receptor alkylation in brain membranes | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Psychiatry | en_US |
dc.subject.hlbsecondlevel | Neurosciences | en_US |
dc.subject.hlbsecondlevel | Chemistry | en_US |
dc.subject.hlbsecondlevel | Biological Chemistry | en_US |
dc.subject.hlbtoplevel | Science | 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, The University of Michigan Medical School, Ann Arbor, Michigan 48109, U.S.A. | en_US |
dc.contributor.affiliationum | Departments of Biological Chemistry and Pharmacology, The University of Michigan Medical School, Ann Arbor, Michigan 48109, U.S.A. | en_US |
dc.identifier.pmid | 2830555 | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/26499/1/0000035.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0028-3908(87)90129-8 | en_US |
dc.identifier.source | Neuropharmacology | 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.