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ACTIVITY AND TOXICITY OF ANESTHETIC-ANALGESIC AGENTS IN TERMS OF MEMBRANE INTERACTION AS ONE OF PHARMACOLOGICAL MECHANISMS
https://asahi-u.repo.nii.ac.jp/records/7258
https://asahi-u.repo.nii.ac.jp/records/7258f7f2ae40-19d5-4bf3-88f3-e4d6324b4b86
| Item type | 朝日大学 教育・研究業績(1) | |||||
|---|---|---|---|---|---|---|
| 公開日 | 2017-10-12 | |||||
| タイトル | ||||||
| タイトル | ACTIVITY AND TOXICITY OF ANESTHETIC-ANALGESIC AGENTS IN TERMS OF MEMBRANE INTERACTION AS ONE OF PHARMACOLOGICAL MECHANISMS | |||||
| 言語 | ||||||
| 言語 | eng | |||||
| 資源タイプ | ||||||
| 資源タイプ識別子 | http://purl.org/coar/resource_type/c_1843 | |||||
| 資源タイプ | other | |||||
| アクセス権 | ||||||
| アクセス権 | metadata only access | |||||
| アクセス権URI | http://purl.org/coar/access_right/c_14cb | |||||
| 業績分類 | ||||||
| 値 | 学会発表 | |||||
| 教員氏名 |
土屋, 博紀
× 土屋, 博紀 |
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| 発行、発表雑誌等、又は発表学会等の名称 | ||||||
| 値 | The 13rd Asian and Oceanic Society of Regional Anesthesia and Pain Medicine Congress (Bangkok, Thailand) | |||||
| 単著、共著の別 | ||||||
| 値 | 共同発表 | |||||
| 発行又は発表の年月 | ||||||
| 日付 | 2015-01-23 | |||||
| 概要 | ||||||
| 値 | Drugs used for pain relief possibly act on membrane lipids besides target proteins. As one pharmacological mechanism in common with them, we studied the interactions of selected anesthetic-analgesic agents with lipid bilayer membranes by paying attention to their clinically relevant concentrations and stereostructure specificity. Unilamellar vesicles suspended in buffer were prepared with phospholipids and cholesterol to mimic the membrane lipid compositions of neuronal and myocardial cells. The membrane preparations were treated with anesthetics, phenolic analgesics, non-steroidal anti-inflammatory drugs and NMDA receptor antagonist at 1–200 μM, followed by measuring fluorescence polarization to determine their induced changes in membrane fluidity. All the tested drugs acted on membrane lipid bilayers to modify their fluidity. Local anesthetic lidocaine, bupivacaine and ropivacaine; phenolic analgesic or anesthetic thymol, eugenol, guaiacol and propofol; and NMDA receptor antagonist ketamine increased the membrane fluidity at anesthetic, nerve-sedative or cardiotoxic concentrations, whereas anti-inflammatory ibuprofen and indomethacin decreased the membrane fluidity at analgesic concentrations. In the biomimetic membranes consisting of chiral cholesterol, stereoisomers showed the enantiomer-specific membrane interactions with the potencies being R(+)- > racemic > S(–)-bupivacaine, S(+)- > racemic ketamine, and S(+)- > racemic > R(–)-ibuprofen, which agreed with those of their relative toxic or analgesic effects. Anesthetic-analgesic agents interact with lipid bilayer membranes in common, thereby directly affecting the functions of biomembranes and indirectly modulating the activities of ion channels, receptors and enzymes through the conformational changes of membrane-embedded proteins. The membrane physicochemical modification may explain the diversity in their pharmacological properties. | |||||
