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Butorphanol: Effects of a Prototypical Agonist-Antagonist Analgesic on .KAPPA.-Opioid Receptors
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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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- Ho Ing K.
- Department of Pharmacology & Toxicology, University of Mississippi Medical Center
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- Rockhold Rob W.
- Department of Pharmacology & Toxicology, University of Mississippi Medical Center
Bibliographic Information
- Other Title
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- Butorphanol: Effects of a Prototypical Agonist-Antagonist Analgesic, on κ-Opioid Receptors
- Butorphanol Effects of a Prototypical Agonist Antagonist Analgesic on カッパ Opioid Receptors
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Description
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.<br>
Journal
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- Journal of Pharmacological Sciences
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Journal of Pharmacological Sciences 98 (2), 109-116, 2005
The Japanese Pharmacological Society
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Keywords
Details 詳細情報について
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- CRID
- 1390282680152514816
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- NII Article ID
- 10025728151
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- NII Book ID
- AA11806667
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- ISSN
- 13478648
- 13478613
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- NDL BIB ID
- 7337818
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- PubMed
- 15942128
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- Text Lang
- en
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- Article Type
- journal article
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- Data Source
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- JaLC
- NDL Search
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed