Journal article
Relative efficacies of δ-opioid receptor agonists at the cloned human δ-opioid receptor
European journal of pharmacology, Vol.326(1), pp.101-104
1997
Handle:
https://hdl.handle.net/2376/110084
PMID: 9178661
Abstract
The present study was conducted to determine the relative efficacies of the selective δ-opioid receptor agonists SNC80 ((+)-4-[(α
R)-α-((2
S,5
R)-4-allyl-2,5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-
N,
N-diethylbenzamide), pCl-DPDPE (cyclic[
d-Pen
2,4′-ClPhe
4,
d-Pen
5]enkephalin) and (−)-TAN67 ((−)-2-methyl-4
aα-(3-hydroxyphenyl)-1,2,3,4,4
a,5,12,12
aα-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]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
max)(
A′/
A+1)×0.5. Results show that SNC80 and pCl-DPDPE had efficacy values that were about 6–7 times greater than that of (−)-TAN67.
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Details
- Title
- Relative efficacies of δ-opioid receptor agonists at the cloned human δ-opioid receptor
- Creators
- Raymond M Quock - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USAYoshiaki Hosohata - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USARichard J Knapp - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USAThomas H Burkey - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USAKeiko Hosohata - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USAXiaoyan Zhang - Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USAKenner C Rice - Laboratory of Medicinal Chemistry, National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, Bethesda, MD 20892, USAHiroshi Nagase - Basic Research Laboratory, Toray Industries, Inc., Kamakura 248, JapanVictor J Hruby - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USAFrank Porreca - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USAWilliam R Roeske - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USAHenry I Yamamura - Departments of Pharmacology, Biochemistry, Psychiatry, and Chemistry and the Program in Neuroscience, University of Arizona, Tucson, AZ 85724, USA
- Publication Details
- European journal of pharmacology, Vol.326(1), pp.101-104
- Academic Unit
- Psychology, Department of
- Publisher
- Elsevier B.V
- Identifiers
- 99900547142801842
- Language
- English
- Resource Type
- Journal article