Bremazocine Recognizes the Difference in Four Amino Acid Residues to Discriminate Between a Nociceptin/Orphanin FQ Receptor and Opioid Receptors
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概要
- 論文の詳細を見る
We investigated the molecular basis of the discrimination between nociceptin/orphanin FQ receptor (NociR) and opioid receptors (OPRs) by bremazocine, a non-type-selective opioid ligand. Construction of several chimeric receptors between NociR and κ-opioid receptor (KOPR) and mutant NociRs followed by binding experiments with [3H]bremazocine showed that the mutation of only four amino acid residues of NociR, Ala216, Val279, Gln280 and Val281, to the amino acid residues located at the corresponding position of KOPR, Lys227, Ile290, His291 and Ile292, made it possible for the resultant mutant NociR to bind bremazocine with high affinity. Considering that these four amino acid residues are conserved among μ-, δ- and κ-OPRs, the present result suggests that bremazocine recognizes the difference in these four amino acid residues to discriminate between NociR and OPRs.
- 社団法人 日本薬理学会の論文
- 1998-08-01
著者
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SEKI Takahiro
Department of Molecular and Pharmacological Neuroscience, Graduate School of Biomedical Sciences, Hi
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Uehara Tomoya
Department of Molecular Imaging and Radiotherapy, Chiba University Graduate School of Pharmaceutical
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Seki Takahiro
Department Of Molecular And Pharmacological Neuroscience Graduate School Of Biomedical Sciences Hiro
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NAKAGAWA Takayuki
Department of Molecular Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University
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Uehara Tomoya
Department Of Molecular Imaging And Radiotherapy Chiba University Of Pharmaceutical Sciences
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Uehara Tomoya
Department Of Molecular Pharmacology Faculty Of Pharmaceutical Sciences Kyoto University
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Seki Takahiro
Department Of Molecular Pharmacology Faculty Of Pharmaceutical Sciences Kyoto University
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SATOH Masamichi
Department of molecular Pharmacology, Faculty of Pharmaceutical Sciences, Kyoto university
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Nakagawa Takayuki
Department Of Molecular Pharmacology Graduate School Of Pharmaceutical Sciences Kyoto University
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Nakagawa Takayuki
Department Of Fisheries Faculty Of Agriculture Kinki University
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Kimura Chiaki
Department Of Molecular Pharmacology Faculty Of Pharmaceutical Sciences Kyoto University
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MINAMI Masabumi
Department of Molecular Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University
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Minami Masabumi
Department Of Molecular Pharmacology Faculty Of Pharmaceutical Sciences Kyoto University
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Nakagawa Takayuki
Dep. Of Molecular Pharmacology Graduate School Of Pharmaceutical Sciences Kyoto Univ. Jpn
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Seki T
Department Of Molecular Pharmacology Faculty Of Pharmaceutical Sciences Kyoto University
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Satoh Masamichi
Department Of Molecular Pharmacology Faculty Of Pharmaceutical Science Kyoto University
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Satoh Masamichi
Yasuda Women's Univ. Jpn
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Sato Masamichi
Department Of Hygiene And Preventive Medicine Faculty Of Medicine Saitama Medical School
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Seki Takahiro
Department Of Computer Science Tokyo Institute Of Technology:(present Address)ibm Global Service-jap
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Satoh Masamichi
Department Of Hygiene And Preventive Medicine Faculty Of Medicine Saitama Medical School
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Seki Takahiro
Department Of Applied Physics Nagoya University
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