Butorphanol : Effects of a Prototypical Agonist-Antagonist Analgesic on κ-Opioid Receptors
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概要
- 論文の詳細を見る
The opioid analgesic, butorphanol (17-cyclobutylmethyl-3,14-dihydroxymorphinan) tartrate is a prototypical agonist-antagonist opioid analgesic agent whose potential for abuse has been the cause of litigation in the United States. With a published affinity for opioid receptors in vitro of 1:4:25 (μ:δ:κ), the relative contribution of actions at each of these receptors to the in vivo actions of the drug are an issue of active investigation. A body of evidence has been developed which indicates that a substantial selective action of butorphanol on the κ-opioid receptor mediates the development of tolerance to butorphanol and cross-tolerance to other opioid agonists; to the production of dependence upon butorphanol, particularly in the rodent; and to compensatory alterations in brain opioid receptor-effector systems. This perspective will identify the current state of understanding of the effects produced by butorphanol on brain opioid receptors, particularly on the κ-opioid receptor subtype, and on the expression of phosphotyrosyl proteins following chronic treatment with butorphanol.
- 社団法人 日本薬理学会の論文
- 2005-06-20
著者
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HO Ing
Department of Pharmacology and Toxicology, University of Mississippi Medical Center
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Ho Ing
Department Of Pharmacology & Toxicology University Of Mississippi Medical Center
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COMMISKEY Stephen
Department of Pharmacology & Toxicology, University of Mississippi Medical Center
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FAN Lir-Wan
Department of Pharmacology & Toxicology, University of Mississippi Medical Center
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ROCKHOLD Rob
Department of Pharmacology & Toxicology, University of Mississippi Medical Center
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Fan Lir-wan
Department Of Pharmacology & Toxicology University Of Mississippi Medical Center
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Rockhold Rob
Department Of Pharmacology & Toxicology University Of Mississippi Medical Center
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Commiskey Stephen
Department Of Pharmacology & Toxicology University Of Mississippi Medical Center
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