Relative efficacies of delta-opioid receptor agonists at the cloned human delta-opioid receptor.
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.
Quock
R M
RM
Department of Pharmacology, University of Arizona, Tucson 85724, USA.
Hosohata
Y
Y
Knapp
R J
RJ
Burkey
T H
TH
Hosohata
K
K
Zhang
X
X
Rice
K C
KC
Nagase
H
H
Hruby
V J
VJ
Porreca
F
F
Roeske
W R
WR
Yamamura
H I
HI
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
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