Evidence for the Existence of the β-Endorphin-Sensitive "ε-Opioid Receptor" in the Brain: The Mechanisms of ε-Mediated Antinociception
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概要
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Recently, μ-, δ- and κ-opioid receptors have been cloned and relatively well-characterized. In addition to three major opioid receptor types, more extensive studies have suggested the possible existence of other opioid receptor types that can be classified as non-μ, non-δ and non-κ. Based upon anatomical and binding studies in the brain, the sensitive site for an endogenous opioid peptide, β-endorphin, has been postulated to account for the unique characteristics of the opioid receptor defined as a putative ε-opioid receptor. Many ε-opioid receptors are functionally coupled to G-proteins. The functional ε-opioid receptors in the brain are stimulated by bremazocine and etorphine as well as β-endorphin, but not by selective μ-, δ- or κ-opioid receptor agonists. ε-Opioid receptor agonists injected into the brain produce profound antinociception. The brain sites most sensitive to ε-agonist-induced antinociception are located in the caudal medial medulla such as the nucleus raphe obscures, nucleus raphe pallidus and the adjacent midline reticular formation. The stimulation of ε-opioid receptors in the brain facilitates the descending enkephalinergic pathway, which probably originates from the brainstem terminating at the spinal cord. The endogenous opioid Met-enkephalin, released in the spinal cord by activation of supraspinal ε-opioid receptors, stimulates spinal δ2-opioid receptors for the production of antinociception. It is noteworthy that the ε-opioid receptor-mediated pain control system is different from that of other opioid systems. Although there appears to be no ε-selective ligand currently available, these findings provide strong evidence for the existence of the putative ε-opioid receptor and its unique function in the brain.
- 社団法人 日本薬理学会の論文
著者
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Tseng Leon
Department Of Anesthesiology Medical College Of Wisconsin
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NARITA Minoru
Department of Toxicology, School of Pharmacy, Hoshi University
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Narita Minoru
Department Of Emergency Medicine Tokyo Women's Medical University
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Narita Minoru
Department Of Anesthesiology Medical College Of Wisconsin
関連論文
- Recent Advances in the Search for the μ-Opioidergic System : Preface
- Morphine, Oxycodone, and Fentanyl Exhibit Different Analgesic Profiles in Mouse Pain Models
- S2-3 Opiate Psychotoxicity : role of NMDA recepter subunits and protein kinase C(Proceedings of the 27th Annual Meeting)
- Recent Advances in the Search for the μ-Opioidergic System : The Antinociceptive Properties of Endomorphin-1 and Endomorphin-2 in the Mouse
- Generalization of NMDA-Receptor Antagonists to the Discriminative Stimulus Effects of κ-Opioid Receptor Agonists U-50,488H, but Not TRK-820 in Rats
- Lack of μ-Opioid Receptor-Mediated G-Protein Activation in the Spinal Cord of Mice Lacking Exon 1 or Exons 2 and 3 of the MOR-1 Gene
- TRK-820, a Selective к-Opioid Agonist, Produces Potent Antinociception in Cynomolgus Monkeys
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- Modulation of the Discriminative Stimulus Effects of Cocaine and Methamphetamine by the Histaminergic System
- Evidence for the Existence of the β-Endorphin-Sensitive "ε-Opioid Receptor" in the Brain: The Mechanisms of ε-Mediated Antinociception
- Hyperactivity in novel environment with increased dopamine and impaired novelty preference in apoptosis signal-regulating kinase 1 (ASK1)-deficient mice
- S9-4 Molecular mechanism of changes in the morphine-induced rewarding effect under chronic pain-like state : Suppression of dopaminergic transmission in the brain(SYMPOSIUM 9: MOLECULAR MECHANISMS OF DRUG DEPENDENCE)(Proceedings of the 31st Annual Meeting
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