Characterization of Specific [3H]Nociceptin Binding in Rat Brain and Spinal Cord.

• KUSAKA Toyofumi

  Department of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka

• YAMADA Shizuo

  Department of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka

• KIMURA Ryohei

  Department of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka

抄録

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°C 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°C, 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°C. Nociceptin and its analogue, [Phe¹Ψ(CH₂-NH)-Gly²]nociceptin(1—13)NH₂ 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.

収録刊行物

• Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ

  Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 24 (8), 902-905, 2001

  公益社団法人 日本薬学会

キーワード

• [<SUP>3</SUP>H]nociceptin binding
• brain
• spinal cord

詳細情報

• CRID: 1390001204625175936
• NII論文ID: 110003638585
• NII書誌ID: AA10885497
• DOI: 10.1248/bpb.24.902
• COI: 1:CAS:528:DC%2BD3MXlvVCmsLo%3D
• ISSN: 13475215
• ISSN: 09186158
• NDL書誌ID: 5852139
• PubMed: 11510482
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I5852139
• Web Site: http://www.jstage.jst.go.jp/article/bpb/24/8/24_8_902/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2002001493
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可