Interactions between Local Anesthetics and Na〔+〕 Channel Inactivation Gate Peptides in Phosphatidylserine Suspensions as Studied by 1H-NMR Spectroscopy
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- タイトル別名
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- Interactions between Local Anesthetics and Na+ Channel Inactivation Gate Peptides in Phosphatidylserine Suspensions as Studied by 1H-NMR Spectroscopy.
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説明
Interactions between local anesthetics and a sodium channel inactivation gate peptide (Ac-GGQDIFMTEEQK-NH2, 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.
収録刊行物
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- ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ
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ＣＨＥＭＩＣＡＬ ＆ ＰＨＡＲＭＡＣＥＵＴＩＣＡＬ ＢＵＬＬＥＴＩＮ 48 (9), 1293-1298, 2000
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679140013568
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- NII論文ID
- 130003948199
- 110003635648
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- NII書誌ID
- AA00602100
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- COI
- 1:CAS:528:DC%2BD3cXmsVeku7g%3D
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 5508130
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- PubMed
- 10993227
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- 本文言語コード
- en
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- 資料種別
- journal article
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- データソース種別
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- JaLC
- NDLサーチ
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- PubMed
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- 使用不可