Compertitive Inhibition of Δ^8-Tetrahydrocannabinol and Its Active Metabolites for Cannabinoid Receptor Binding

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概要

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• In vitro binding characteristics of Δ^8-tetrahydrocannabinol (Δ^8-THC) and its metabolites, 11-hydroxy-Δ^8-THC (11-OH-Δ^8-THC) and 11-oxo-Δ^8-THC, as well as an inactive metabolite, Δ^8-THC-11-oic acid, as a cannabinoid receptor site from bovine cortex were examined using the specific agonist [^3H]CP-55940. 11-OH-Δ^8-THC and 11-oxo-Δ^8-THC strongly inhibited the specific binding of [^3H]CP-55940. The K_i values of 11-OH-Δ^8-THC and 11-oxo-Δ^8-THC for the specific binding of [^3H]CP-55940 were 52 and 143 nM, respectively, whereas that of Δ^8-THC-11-oic acid was 917 nM. Scatchard plot analyses indicated that 11-OH-Δ^8-THC and 11-oxo-Δ^8-THC caused a significant increase in the apparent K_D value without changing the apparent B_<max>. These results reveal that active metabolites of Δ^8-THC also competitively bind to the cannabinoid receptor as agonists.

• 公益社団法人日本薬学会の論文
• 1998-04-15

著者

• YAMAMOTO IKUO

  Department of Laboratory Medicine, Miyazaki Medical College

• 景山 節

  京大・霊長類研・生化学

• Yamamoto Ikuo

  Department Of Hygienic Chemistry School Of Pharmaceutical Sciences Kyushu University Of Health And W

• Kimura Toshiyuki

  Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University

• Watanabe Kazuhito

  Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University

• HO Ing

  University of Mississippi Medical Center

• HO Ing

  Department of Pharmacology and Toxicology, University of Mississippi Medical Center

• YOSHIDA Hisatoshi

  Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University

• Yamamoto Ikuo

  北陸大学 薬 衛化

• Yamamoto Ikuo

  Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University

• YAMAMOTO IKUO

  Hygienic Chemistry

• Kimura T

  Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University

• KAMEI Ayako

  Department of Hygienic Chemistry, Faculty of Pharmaceutical Sciences, Hokuriku University

• 景山 節

  京都大学霊長類研究所人類進化モデル研究センター

• 景山 節

  京大・霊長研

• Ho Ing

  ミシシッピ大学医学部薬毒理学教室

• Kimura Toshiyuki

  Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University

• Watanabe Kazuhito

  Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University

• Watanabe Kazuhito

  Department Of Chemistry And Chemical Engineering Faculty Of Engineering Yamagata University

• Yoshimura Hidetoshi

  Faculty Of Pharmaceutical Sciences Kyushu University(present):department Of Food And Nutrition Nakam

• Kimura T

  Department Of Medicinal Chemistry Center For Frontier Research In Medicinal Science 21st Century Coe

• Ho Ing

  Department Of Pharmacology & Toxicology University Of Mississippi Medical Center

• Kamei Ayako

  Department Of Hygienic Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University

• Yoshida H

  Lab. Of Food & Nutritional Sciences Dep. Of Nutritional Sci. Kobe-gakuin Univ.

• Yamamoto I

  Hygienic Chemistry

• Yoshida Hiromi

  Department Of Nutritional Science Kobe Gakuin University

• Watanabe Kazuhito

  Faculty Of Pharmaceutical Sciences Kyushu University

• Yamamoto Ikuo

  Department Of Bioapplied Chemistry Faculty Of Engineering Osaka City University

• Kimura T

  Peptide Inst. Inc. Minoh Jpn

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