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Vol. 51, Issue 3, 503-532, September 1999
-Opioid Receptor: Molecular Pharmacology, Signal
Transduction, and the Determination of Drug Efficacy
Department of Pharmaceutical Sciences, Washington State University
College of Pharmacy, Pullman, Washington (R.M.Q.); Department of
Pharmacology, University of California-Irvine College of Medicine,
Irvine, California (F.J.E.); and Departments of Pharmacology (T.H.B.,
E.V., Y.H., K.H., S.C., C.S., W.R.R., H.I.Y.), Biochemistry (H.I.Y.),
Medicine (W.R.R.), and Psychiatry (H.I.Y.) and the Program in
Neuroscience (W.R.R., H.I.Y.), University of Arizona Health Sciences
Center, Tucson, Arizona
I. Introduction
II. Role of 
-Opioid Receptors in Antinociception
III. The -Opioid Receptor
A. Endogenous 
-Opioid Receptors
B. Cloned -Opioid Receptors
IV. Molecular Biology of -Opioid Receptors
A. Antisense Oligodeoxynucleotide Gene Knockdown
B. Receptor Knockout Studies in Transgenic Animals
C. Identification of -Opioid Receptor Domains Mediating Receptor
Function
1. Identification of Ligand-Binding Domains.
2. -Opioid Receptor Domains Mediating Down-Regulation.
3. -Opioid Receptor Domains Mediating Signal Transduction
Cascades.
V. Opioid Signal Transduction
A. G Protein Activity
B. -Opioid Receptors Inhibit cAMP Production in Cells and
Tissues
C. Protein Kinases
D. Ion Channels
1. Calcium Flux.
2. K+ Conductance.
E. Summary
VI. -Opioid Receptor-Selective Agonist Efficacy
A. Evolution of the Concept of Efficacy
1. Ariëns' Concept of Intrinsic Activity.
2. Stephenson's Concept of Efficacy.
3. Furchgott's Concept of Intrinsic Efficacy.
4. Estimation of Relative Efficacy Using the Formula of
Ehlert.
5. Summary.
B. Relative Efficacy of -Selective Drugs in Transfected Cells
That Stably Express the Human -Opioid Receptor
1. -Opioid Receptor-Selective Agonists.
2. Comparison of Stephenson Efficacy and Ehlert Relative Efficacy
Calculations.
3. Summary: Drug Efficacy Determinations in Transfected Cell
Lines.
VII. Conclusions and Future Directions
Acknowledgments
References
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