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Analgesic Agents Share the Membrane Interactivity Possibly Associated with the Diversity of Their Pharmacological Properties
https://asahi-u.repo.nii.ac.jp/records/7260
https://asahi-u.repo.nii.ac.jp/records/72601fdbde03-8663-4621-ac5e-1491098877ad
| 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 | Analgesic Agents Share the Membrane Interactivity Possibly Associated with the Diversity of Their Pharmacological Properties | |||||
| 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 | 学術雑誌論文 | |||||
| 教員氏名 |
土屋, 博紀
× 土屋, 博紀 |
|||||
| 発行、発表雑誌等、又は発表学会等の名称 | ||||||
| 値 | British Journal of Pharmaceutical Research | |||||
| 巻 | ||||||
| 値 | 7 | |||||
| 号 | ||||||
| 値 | 2 | |||||
| 掲載ページ | ||||||
| 値 | pp. 110-121 | |||||
| 単著、共著の別 | ||||||
| 値 | 共著 | |||||
| 発行又は発表の年月 | ||||||
| 日付 | 2015-06-01 | |||||
| ISSN | ||||||
| 値 | 2231-2919 | |||||
| PubMed番号 | ||||||
| 値 | doi: 10.9734/BJPR/2015/18269 | |||||
| 概要 | ||||||
| 値 | Various drugs used for pain relief show the diversity of pharmacological properties besides their intrinsic analgesic activity. In order to verify a common mechanism, we studied the effects of selected analgesic agents on lipid bilayer membranes by paying attention to their induced physicochemical membrane modification and stereostructure specificity. All the tested drugs interacted with lipid bilayer membranes to modify their fluidity. Lidocaine, bupivacaine, ropivacaine, thymol, eugenol, guaiacol, propofol and ketamine increased the fluidity of neuronal mimetic membranes at 0.1-200 μM, whereas ibuprofen and indomethacin decreased the membrane fluidity at 100-200 μM. In neuronal and myocardial mimetic membranes consisting of 35-40 mol% chiral cholesterol, stereoisomers (25-200 μM) showed the enantiomerspecific membrane effects with the relative potencies being R(+)-bupivacaine > racemic bupivacaine > S(–)-bupivacaine, S(+)-ketamine > racemic ketamine, and S(+)-ibuprofen > racemic ibuprofen > R(–)-ibuprofen, which were correlated with those of their analgesic, anesthetic or cardiotoxic effects. Analgesic agents share the ability to interact with lipid bilayers, directly influencing the properties and functions of biomembranes at a lipid level and indirectly modulating the activities of membrane-associated ion channels, receptors and enzymes through the conformational changes of proteins. The membrane interactivity possibly accounts for their pharmacological diversity. | |||||
