TY - JOUR
T1 - Relative efficacies of 6-opioid receptor agonists at the cloned human δ-opioid receptor
AU - Quock, Raymond M.
AU - Hosohata, Yoshiaki
AU - Knapp, Richard J.
AU - Burkey, Thomas H.
AU - Hosohata, Keiko
AU - Zhang, Xiaoyan
AU - Rice, Kenner C.
AU - Nagase, Hiroshi
AU - Hruby, Victor J.
AU - Porreca, Frank
AU - Roeske, William R.
AU - Yamamura, Henry I.
PY - 1997/5/12
Y1 - 1997/5/12
N2 - The present study was conducted to determine the relative efficacies of the selective δ-opioid receptor agonists SNC80((+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3- S,5 R) -4-allyl-2,5-dimethyl-1-piherazinyl)-3-methoxybenzyl]-N,N- diethylbenzamide), pCl-DPDPE (cyclic[D-Pen2,4'-ClPhe4,D-Pen5]enkephalin) and (-)-TAN67 ((-)-2-methyl-4aα-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12aα-octahyhro-quinolino -[2,3,3-g]isoquinoline). Experiments compared the abilities of the three drugs to competitively inhibit [3H]naltrindole binding and also stimulate [35S]GTPγS binding in membranes prepared from stably transfected Chinese hamster ovary (CHO) cells that express the cloned human δ-opioid receptor. Efficacy was determined according to the formula: efficacy = (E(max-A)/E(maxi))(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.
AB - The present study was conducted to determine the relative efficacies of the selective δ-opioid receptor agonists SNC80((+)-4-[(αR)-α-((2S,5R)-4-allyl-2,5-dimethyl-1- piperazinyl)-3- S,5 R) -4-allyl-2,5-dimethyl-1-piherazinyl)-3-methoxybenzyl]-N,N- diethylbenzamide), pCl-DPDPE (cyclic[D-Pen2,4'-ClPhe4,D-Pen5]enkephalin) and (-)-TAN67 ((-)-2-methyl-4aα-(3-hydroxyphenyl)-1,2,3,4,4a,5,12,12aα-octahyhro-quinolino -[2,3,3-g]isoquinoline). Experiments compared the abilities of the three drugs to competitively inhibit [3H]naltrindole binding and also stimulate [35S]GTPγS binding in membranes prepared from stably transfected Chinese hamster ovary (CHO) cells that express the cloned human δ-opioid receptor. Efficacy was determined according to the formula: efficacy = (E(max-A)/E(maxi))(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.
KW - Efficacy
KW - Radioligand binding
KW - [S]GTPγS binding
KW - δ-Opioid receptor agonist
KW - δ-Opioid receptor, human
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U2 - 10.1016/S0014-2999(97)83488-7
DO - 10.1016/S0014-2999(97)83488-7
M3 - Article
C2 - 9178661
AN - SCOPUS:0030610216
VL - 326
SP - 101
EP - 104
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 1
ER -