Interactions between Local Anesthetics and Na^+ Channel Inactivation Gate Peptides in Phosphatidylserine Suspensions as Studied by ^1H-NMR Spectroscopy

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概要

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• Interactions between local anesthetics and a sodium channel inactivation gate peptide (Ac-GGQDIFMTEEQK-NH_2,MP-1A), which was dissected from the cytoplasmic linker between domains III and IV of the sodium channel α-subunit (G1484-K1495 in rat brain type IIA), have been studied by ^1H-NMR spectroscopy. Changes in ^1H-NMR chemical shifts of the aromatic proton resonances of dibucaine (pH 7.0) and lidocaine (pH 6.0 and 9.0) in phosphatidylserine (PS) suspensions were observed. The effects of substitution of glutamine (F1489Q; MP-2A) or D-phenylalanine (MP-1A') for L-phenylalanine (F1489) in MP-1A and the effects of substitution of neutral amino acid residues for the corresponding acidic amino acid residues (D1487N, MP-1NA; E1492Q, MP-1QEA; E1493Q, MP-1EQA) in MP-1A, on the aromatic ^1H-NMR cheimcal shift changes of dibucaine and lidocaine were also investigated. From these results it was concluded that : the aromatic ring of phenylalanine of MP-1A and the aromatic ring of the cationic form of dibucaine or lidcaine are interacting by π-π stacking; the tertiary amine nitrogen of dibucaine is interacting electrostatically with D1487,whereas that of lidocaine is interacting with E1492.

• 公益社団法人日本薬学会の論文
• 2000-09-01

著者

• Kuroda Yoshihiro

  Graduate School of Engineering Science, Osaka University

• FUJII Nobutaka

  Graduate School of Pharmaceutical Sciences, Kyoto University

• OTAKA akira

  Graduate School of Pharmaceutical Sciences, Kyoto University

• Otaka Akira

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Miyamoto Kazuhide

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Fujii Nobutaka

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Kuroda Y

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Kuroda Yoshihiro

  Graduate School Of Engineering Science Osaka University

• NAKAGAWA Terumichi

  Graduate School of Pharmaceutical Science, Kyoto University

• TANAKA Kazufumi

  Graduate School of Pharmaceutical Sciences, Kyoto University

• MAEDA Yoshitaka

  Graduate School of Pharmaceutical Sciences, Kyoto University

• ISHIKAWA Junya

  Graduate School of Pharmaceutical Sciences, Kyoto University

• HINATA Ryo-ichi

  Graduate School of Pharmaceutical Sciences, Kyoto University

• Maeda Yoshitaka

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Nakagawa T

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Nakagawa Terumichi

  Graduate School Of Pharmaceutical Science Kyoto University

• Ishikawa J

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Tanaka Kazufumi

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Hinata Ryo-ichi

  Graduate School Of Pharmaceutical Sciences Kyoto University

• Maeda Yoshitaka

  Graduate School of Material Science, University of Hyogo, Kamigori, Hyogo 678-1297, Japan

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