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  1. 教育・研究業績データ
  2. 歯学部

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/7256
dfdcd6c6-991d-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

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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.
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