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Drinking-Related Tetrahydroharmans Counteract the Membrane Effects of Local Anesthetic Lidocaine
https://asahi-u.repo.nii.ac.jp/records/7256
https://asahi-u.repo.nii.ac.jp/records/7256dfdcd6c6-991d-4db1-a8a5-9348adef8cd0
| 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 | Drinking-Related Tetrahydroharmans Counteract the Membrane Effects of Local Anesthetic Lidocaine | |||||
| 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 |
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| 発行、発表雑誌等、又は発表学会等の名称 | ||||||
| 値 | Journal of Drug and Alcohol Research | |||||
| 巻 | ||||||
| 値 | 3 | |||||
| 掲載ページ | ||||||
| 値 | 1-6 | |||||
| 単著、共著の別 | ||||||
| 値 | 共著 | |||||
| 発行又は発表の年月 | ||||||
| 日付 | 2014-12-10 | |||||
| ISSN | ||||||
| 値 | 2090-8334 (Print Ver)/2090-8342 (Online Ver) | |||||
| PubMed番号 | ||||||
| 値 | doi: 10.4303/jdar/235887 | |||||
| 概要 | ||||||
| 値 | There is a general consensus in dentistry that successful local anesthesia is frequently difficult in habitual drinkers and alcoholic patients. Neuro-active tetrahydroharmans increase in human body fluids and tissues by consuming alcoholic beverages. To understand such reduced anesthetic efficacy by the drug interaction hypothesis, we studied the influences of drinking-related tetrahydroharmans on membrane fluidization as one of local anesthetic mechanisms. Liposomal membranes prepared with phosphatidylcholine and cholesterol were treated with lidocaine and different tetrahydroharmans separately and in combination, followed by measuring fluorescence polarization to determine their induced changes in membrane fluidity. In contrast to 0.1–2 mg/mL lidocaine, tetrahydroharmans decreased the fluidity of membrane preparations at -25 μg/mL with the potency being 1,2,3,4-tetrahydroharman ≫ 1,2,3,4-tetrahydronorharman. 1,2,3,4-Tetrahydroharman counteracted the membrane-fluidizing effects of 1 mg/mL lidocaine at physiologically relevant 0.25–2.5 ng/mL, whereas neither its 6-hydroxyl nor 7-hydroxyl metabolite did at 25–200 ng/mL. Such counteraction at a membrane lipid level may be responsible for the reduction of local anesthetic efficacy in drinkers because 1,2,3,4-tetrahydroharman increases in vivo by ingesting alcoholic beverages. | |||||