کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10748406 | 1050274 | 2016 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Emamectin is a non-selective allosteric activator of nicotinic acetylcholine receptors and GABAA/C receptors
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کلمات کلیدی
MCAmaximal currentImaxIVMPTXnAChREC50γ-aminobutyric acid - اسید γ-آمینوبوتیریکEmamectin - امامکتینIvermectin - ایورمکتینEmamectin benzoate - بنزوات امامکتینallosteric activation - فعال شدن آلوستریکMecamylamine - مکامیلامینhalf maximal effective concentration - نیمه حداکثر غلظت موثرPicrotoxin - پیکروتوکسینGABA - گاباnicotinic acetylcholine receptor - گیرنده استیلکولین نیکوتینNicotinic receptor - گیرنده نیکوتین
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Avermectins are a group of compounds isolated from a soil-dwelling bacterium. They have been widely used as parasiticides and insecticides, acting by relatively irreversible activation of invertebrate chloride channels. Emamectin is a soluble derivative of an avermectin. It is an insecticide, which persistently activates glutamate-gated chloride channels. However, its effects on mammalian ligand-gated ion channels are unknown. To this end, we tested the effect of emamectin on two cation selective nicotinic receptors and two GABA-gated chloride channels expressed in Xenopus oocytes using two-electrode voltage clamp. Our results demonstrate that emamectin could directly activate α7 nAChR, α4β2 nAChR, α1β2γ2 GABAA receptor and Ï1 GABAC receptor concentration dependently, with similar potencies for each channel. However, the potencies for it to activate these channels were at least two orders of magnitude lower than its potency of activating invertebrate glutamate-gated chloride channel. In contrast, ivermectin only activated the α1β2γ2 GABAA receptor.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical and Biophysical Research Communications - Volume 473, Issue 4, 13 May 2016, Pages 795-800
Journal: Biochemical and Biophysical Research Communications - Volume 473, Issue 4, 13 May 2016, Pages 795-800
نویسندگان
Xiaojun Xu, Caraline Sepich, Ronald J. Lukas, Guonian Zhu, Yongchang Chang,