title: Relative efficacies of delta-opioid receptor agonists at the cloned human delta-opioid receptor.
abstract: The present study was conducted to determine the relative efficacies of the selective delta-opioid receptor agonists SNC80 ((+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2,5-dimethyl-1-piperazinyl )-3-methoxybenzyl]-N,N-diethylbenzamide), pCl-DPDPE (cyclic[D-Pen2,4'-ClPhe4,D-Pen5]enkephalin) and (-)-TAN67 ((-)-2-methyl-4a alpha-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12a alpha-octahydro-quinolino-[2,3,3-g]isoquinoline). Experiments compared the abilities of the three drugs to competitively inhibit [3H]naltrindole binding and also stimulate [35S]GTPgammaS binding in membranes prepared from stably transfected Chinese hamster ovary (CHO) cells that express the cloned human delta-opioid receptor. Efficacy was determined according to the formula: efficacy = (E(max-A)/Emax)(A'/A + 1) X 0.5. Results show that SNC80 and pCl-DPDPE had efficacy values that were about 6-7 times greater than that of (-)-TAN67.
authors.affiliation: Department of Pharmacology, University of Arizona, Tucson 85724, USA.
authors.forename: R M
authors.initials: RM
authors.lastname: Quock
authors.forename: Y
authors.initials: Y
authors.lastname: Hosohata
authors.forename: R J
authors.initials: RJ
authors.lastname: Knapp
authors.forename: T H
authors.initials: TH
authors.lastname: Burkey
authors.forename: K
authors.initials: K
authors.lastname: Hosohata
authors.forename: X
authors.initials: X
authors.lastname: Zhang
authors.forename: K C
authors.initials: KC
authors.lastname: Rice
authors.forename: H
authors.initials: H
authors.lastname: Nagase
authors.forename: V J
authors.initials: VJ
authors.lastname: Hruby
authors.forename: F
authors.initials: F
authors.lastname: Porreca
authors.forename: W R
authors.initials: WR
authors.lastname: Roeske
authors.forename: H I
authors.initials: HI
authors.lastname: Yamamura
mesh_terms: D000818:Animals; D001549:Benzamides / Q000494:pharmacology; D016466:CHO Cells; D003001:Cloning, Molecular; D006224:Cricetinae; D020881:Enkephalin, D-Penicillamine (2,5)-; D004745:Enkephalins / Q000494:pharmacology; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000378:metabolism; D006801:Humans; D009271:Naltrexone / Q000031:analogs & derivatives / Q000378:metabolism; D009292:Narcotic Antagonists / Q000378:metabolism; D010879:Piperazines / Q000494:pharmacology; D011804:Quinolines / Q000494:pharmacology; D017465:Receptors, Opioid, delta / Q000819:agonists*; D013462:Sulfur Radioisotopes
chemical_list: D001549:Benzamides; D004745:Enkephalins; D009292:Narcotic Antagonists; D010879:Piperazines; D011804:Quinolines; D017465:Receptors, Opioid, delta; D013462:Sulfur Radioisotopes; C094142:TAN 67; C088464:4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D009271:Naltrexone; D020881:Enkephalin, D-Penicillamine (2,5)-; C055382:naltrindole