Differential down-regulation of the human delta-opioid receptor by SNC80 and [D-Pen(2),D-Pen(5)]enkephalin.
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.
Okura
T
T
Departments of Pharmacology, Biochemistry, Medicine, Psychiatry, and the Program in Neuroscience, College of Medicine, University of Arizona Health Sciences Center, Tucson, AZ 85724, USA.
Cowell
S M
SM
Varga
E
E
Burkey
T H
TH
Roeske
W R
WR
Hruby
V J
VJ
Yamamura
H I
HI
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
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