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Lipophilicity of opioids determined by a novel micromethod

dc.contributor.authorMedzihradsky, Fedoren_US
dc.contributor.authorEmmerson, Paul J.en_US
dc.contributor.authorMousigian, Carol A.en_US
dc.date.accessioned2006-04-10T15:16:08Z
dc.date.available2006-04-10T15:16:08Z
dc.date.issued1992-04en_US
dc.identifier.citationMedzihradsky, Fedor, Emmerson, Paul J., Mousigian, Carol A. (1992/04)."Lipophilicity of opioids determined by a novel micromethod." Journal of Pharmacological and Toxicological Methods 27(2): 67-69. <http://hdl.handle.net/2027.42/30114>en_US
dc.identifier.urihttp://www.sciencedirect.com/science/article/B6T8S-475J9C9-9/2/7094c10cf2c151ea335d9a79c4a1d3b9en_US
dc.identifier.urihttps://hdl.handle.net/2027.42/30114
dc.identifier.urihttp://www.ncbi.nlm.nih.gov/sites/entrez?cmd=retrieve&db=pubmed&list_uids=1591405&dopt=citationen_US
dc.description.abstractThe lipophilicity of various [mu]-selective opioids was determined by measuring their distribution between n-octanol and Tris.HCl buffer, pH 7.4, by a procedure requiring submicromolar concentrations (submilligram amounts) of the compounds. After partitioning at 25[deg]C, the concentration of opioids in the aqueous phase was quantified by their displacement of bound [3H]Tyr-Ala-Gly-(Me)Phe-Gly-ol (DAMGO) from opioid receptor in brain membranes. The obtained distribution coefficients (log Papp) agreed well with respective values determined previously with other, less sensitive or more cumbersome, methods of quantitation. The procedure is precise and versatile, and offers the routine assessment of lipophilicity as part of the in vitro characterization of opioids frequently available in limited quantities. In principle, the method is applicable to any compound whose binding to its receptor is quantifiable.en_US
dc.format.extent325451 bytes
dc.format.extent3118 bytes
dc.format.mimetypeapplication/pdf
dc.format.mimetypetext/plain
dc.language.isoen_US
dc.publisherElsevieren_US
dc.titleLipophilicity of opioids determined by a novel micromethoden_US
dc.typeArticleen_US
dc.rights.robotsIndexNoFollowen_US
dc.subject.hlbsecondlevelBiological Chemistryen_US
dc.subject.hlbtoplevelScienceen_US
dc.subject.hlbtoplevelHealth Sciencesen_US
dc.description.peerreviewedPeer Revieweden_US
dc.contributor.affiliationumDepartments of Biological Chemistry and Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, U.S.A.; Departments of Biological Chemistry and Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, U.S.A.en_US
dc.contributor.affiliationumDepartments of Biological Chemistry and Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, U.S.A.; Departments of Biological Chemistry and Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, U.S.A.en_US
dc.contributor.affiliationumDepartments of Biological Chemistry and Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, U.S.A.; Departments of Biological Chemistry and Pharmacology, University of Michigan Medical School, Ann Arbor, Michigan, U.S.A.en_US
dc.identifier.pmid1591405en_US
dc.description.bitstreamurlhttp://deepblue.lib.umich.edu/bitstream/2027.42/30114/1/0000489.pdfen_US
dc.identifier.doihttp://dx.doi.org/10.1016/1056-8719(92)90023-Ten_US
dc.identifier.sourceJournal of Pharmacological and Toxicological Methodsen_US
dc.owningcollnameInterdisciplinary and Peer-Reviewed


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