Abstract
Nonselective opioid partial agonists, such as buprenorphine, butorphanol, and pentazocine, have been widely used as analgesics and for anti-addiction therapy. However, the precise molecular mechanisms underlying the therapeutic and rewarding effects of these drugs have not been clearly delineated. Recent success in developing μ-opioid receptor knockout (MOP-KO) mice has elucidated the molecular mechanisms underlying the effects of morphine and other opioids. We have revealed the in vivo roles of MOPs in the effects of opioid partial agonists by using MOP-KO mice for behavioral tests (e.g., several kinds of antinociceptive tests for analgesic effects, conditioned place preference test for dependence). The combination of the cell culture assays using cDNA for μ, δ, and κ opioid receptors and the behavioral tests using MOP-KO mice has provided novel theories on the molecular mechanisms underlying the effects of opioid ligands, especially opioid partial agonists.
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Acknowledgments
We acknowledge Mr. Michael Arends for his assistance with editing the manuscript. This work was supported by grants from the Ministry of Health, Labour and Welfare of Japan (H17-Pharmaco-001, H19-Iyaku-023), the Ministry of Education, Culture, Sports, Science and Technology of Japan (19603021, 20390162, 19659405).
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Ide, S., Minami, M., Sora, I., Ikeda, K. (2010). Combination of Cell Culture Assays and Knockout Mouse Analyses for the Study of Opioid Partial Agonism. In: Szallasi, A. (eds) Analgesia. Methods in Molecular Biology, vol 617. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-60327-323-7_27
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DOI: https://doi.org/10.1007/978-1-60327-323-7_27
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