کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9921484 | 1559224 | 2005 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Cholinergic drugs potentiate human nicotinic α4β2 acetylcholine receptors by a competitive mechanism
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موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Cholinergic drugs potentiate human nicotinic α4β2 acetylcholine receptors by a competitive mechanism Cholinergic drugs potentiate human nicotinic α4β2 acetylcholine receptors by a competitive mechanism](/preview/png/9921484.png)
چکیده انگلیسی
Effects of cholinergic drugs on human α4β2 nicotinic acetylcholine receptors expressed in Xenopus oocytes have been investigated in electrophysiological and ligand binding experiments. Atropine, scopolamine, physostigmine, and tacrine combine potentiation of ion current induced by low concentrations of acetylcholine with inhibition of ion current evoked by high concentrations of acetylcholine. Rivastigmine, galanthamine, and dichlorvos cause only inhibition of ion current evoked by low concentrations of acetylcholine. Binding experiments show that the potentiating cholinergic drugs atropine, scopolamine, and physostigmine are competitive ligands of human α4β2 nicotinic acetylcholine receptors. Conversely, the inhibitory cholinergic drugs galanthamine and rivastigmine are non-competitive. The non-competitive drugs are not allosteric, since they do not affect the saturation curve of the radioligand [3H]cytisine. Effects of potentiating cholinergic drugs on nicotinic acetylcholine receptors are consistent with and predicted by a model comprising competitive drug effects at two equivalent agonist recognition sites on the nicotinic acetylcholine receptor combined with non-competitive ion channel block.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 509, Issues 2â3, 21 February 2005, Pages 97-108
Journal: European Journal of Pharmacology - Volume 509, Issues 2â3, 21 February 2005, Pages 97-108
نویسندگان
Chantal J.G.M. Smulders, Ruud Zwart, Isabel Bermudez, Regina G.D.M. van Kleef, Paul J. Groot-Kormelink, Henk P.M. Vijverberg,