Characterization of Specific[^3H]Nociceptin Binding in Rat Brain and Spinal Cord
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概要
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The present study was undertaken to characterize simultaneously[^3H]nociceptin binding to opioid receptor-like 1(ORL1)receptors in the rat brain and spinal cord. Specific binding of [^3H]nociceptin to crude membranes from the rat brain and spinal cord at 25℃ was saturable, reversible and of high affinity, and it also exhibited a pharmacological specificity involving the ORL1 receptor. The K_d and B_<max> values for [^3H]nociceptin in the spinal cord were significantly lower than those in the brain. At 4℃, there was a significant increase in the dissociation constant(K_d)for[^3H]nociceptin in the brain and spinal cord with little change in the maximal number of binding sites(B_<max>)compared with that at 25℃. Nociceptin and its analogue, [Phe^1Ψ(CH_2-NH)-Gly^2]nociceptin(1-13)NH_2 were found to be potent inhibitors of[^3H]nociceptin binding to crude membranes from the brain and spinal cord, while opioid ligands such as naloxone-benzoylhydrazone, naltrindole and nor-binaltorphimine, exhibited an inhibitory effect only at high concentrations. The K_i values for nociceptin, its analogue and opioid ligands in the spinal cord were significantly lower than those in the brain. There were regional variations in the specific[^3H]nociceptin binding to crude membranes from the rat brain : a relatively high density of[^3H]nociceptin binding in the cerebral cortex, hippocampus, thalamus and midbrain, moderately dense binding in the corpus striatum and pons/medulla oblongata, and the lowest density of binding in the cerebellum. In conclusion, the present study has shown that[^3H]nociceptin binds selectively to ORL1 receptors in the rat brain and spinal cord.
- 公益社団法人日本薬学会の論文
- 2001-08-01
著者
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YAMADA Shizuo
Department of Pharmacokinetics and Pharmacodynamics and Global Center of Excellence (COE) Program, S
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KIMURA Ryohei
Department of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka
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Yamada Shizuo
Department Of Biophamacy School Of Pharmaceutical Sciences University Of Shizuoka
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Kimura Ryohei
Department Of Biophamacy School Of Pharmaceutical Sciences University Of Shizuoka
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KUSAKA Toyofumi
Department of Biophamacy, School of Pharmaceutical Sciences, University of Shizuoka
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Kusaka Toyofumi
Department Of Biophamacy School Of Pharmaceutical Sciences University Of Shizuoka
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