کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9021453 | 1561374 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Cation-Ï interactions modulate the NMDA receptor inhibitory potencies of inhaled aromatic anesthetics
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شناسی مولکولی
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چکیده انگلیسی
Electrostatic interactions are being increasingly recognized as important modulators of anesthetic action. By virtue of their Ï electron clouds, aromatic anesthetics may engage in attractive electrostatic interactions with cationic atomic charges on protein targets. In this study, we tested the hypothesis that anesthetics containing Ï electron clouds inhibit human N-methyl-d-aspartate (NMDA) receptors with potencies that correlate with their abilities to engage in cation-Ï interactions. Electrophysiological techniques were used to define the NMDA receptor inhibitory potencies of anesthetics containing Ï electron clouds and computer modeling was used to quantify their abilities to engage in cation-Ï interactions. All 18 anesthetics inhibited human NR1/NR2B NMDA receptors reversibly and in a concentration-dependent manner. NMDA receptor inhibitory potency correlated strongly with the ability to engage in cation-Ï interactions and weakly with hydrophobicity. These results provide strong evidence that electrostatic cation-Ï interactions modulate the NMDA receptor inhibitory potencies of volatile anesthetics possessing Ï electron clouds. It suggests that the NMDA receptor inhibitory site for such anesthetics contains a positive charge and that computational modeling may be used to predict the NMDA receptor inhibitory potencies of volatile compounds.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: International Congress Series - Volume 1283, November 2005, Pages 85-89
Journal: International Congress Series - Volume 1283, November 2005, Pages 85-89
نویسندگان
D.E. Raines,