title: Differential down-regulation of the human delta-opioid receptor by SNC80 and [D-Pen(2),D-Pen(5)]enkephalin.
abstract: We examined the contribution of the human delta-opioid receptor carboxyl terminal tail to (+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2, 5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC80)- and cyclic[D-Pen(2),D-Pen(5)]enkephalin (DPDPE)-mediated receptor down-regulation. Both SNC80 and DPDPE mediated down-regulation of an epitope tagged human delta-opioid receptor. Truncation of the human delta-opioid receptor after Gly(338) blocked DPDPE-mediated down-regulation. However, SNC80 mediated significant down-regulation of the truncated receptor. These findings suggest that SNC80-mediated down-regulation involves receptor domains in addition to the carboxyl terminal tail.
authors.affiliation: Departments of Pharmacology, Biochemistry, Medicine, Psychiatry, and the Program in Neuroscience, College of Medicine, University of Arizona Health Sciences Center, Tucson, AZ 85724, USA.
authors.forename: T
authors.initials: T
authors.lastname: Okura
authors.forename: S M
authors.initials: SM
authors.lastname: Cowell
authors.forename: E
authors.initials: E
authors.lastname: Varga
authors.forename: T H
authors.initials: TH
authors.lastname: Burkey
authors.forename: W R
authors.initials: WR
authors.lastname: Roeske
authors.forename: V J
authors.initials: VJ
authors.lastname: Hruby
authors.forename: H I
authors.initials: HI
authors.lastname: Yamamura
mesh_terms: D001549:Benzamides / Q000494:pharmacology*; D015536:Down-Regulation; D020881:Enkephalin, D-Penicillamine (2,5)- / Q000494:pharmacology*; D006801:Humans; D009271:Naltrexone / Q000031:analogs & derivatives / Q000378:metabolism; D010879:Piperazines / Q000494:pharmacology*; D017465:Receptors, Opioid, delta / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism
chemical_list: D001549:Benzamides; D010879:Piperazines; D017465:Receptors, Opioid, delta; C088464:4-(alpha-(4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl)-N,N-diethylbenzamide; D009271:Naltrexone; D020881:Enkephalin, D-Penicillamine (2,5)-; C055382:naltrindole