کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584735 | 981347 | 2012 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Competitive antagonism of insect GABA receptors by iminopyridazine derivatives of GABA
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کلمات کلیدی
SBPFMPFLIPRGABA-gated chloride channelγ-aminobutyric acid - اسید γ-آمینوبوتیریکCompetitive antagonism - انطباق رقابتیInsect - حشرهInsecticide - حشرهکشAmerican cockroach - سوسک آمریکاییFLuorometric Imaging Plate Reader - فلورومتریک تصویربرداری صفحات خوانندهsmall brown planthopper - قهوه ای کوچک قهوه ایCommon cutworm - کرم کرم مشترکGABA - گاباGABA receptor - گیرنده GABA
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of 4-(6-imino-3-aryl/heteroarylpyridazin-1-yl)butanoic acids were synthesized and examined for antagonism of GABA receptors from three insect species. When tested against small brown planthopper GABA receptors, the 3,4-methylenedioxyphenyl and the 2-naphthyl analogues showed complete inhibition of GABA-induced fluorescence changes at 100 μM in assays using a membrane potential probe. Against common cutworm GABA receptors, these analogues displayed approximately 86% and complete inhibition of GABA-induced fluorescence changes at 100 μM, respectively. The 4-biphenyl and 4-phenoxyphenyl analogues showed moderate inhibition at 10 μM in these receptors, although the inhibition at 100 μM was not complete. Against American cockroach GABA receptors, the 4-biphenyl analogue exhibited the greatest inhibition (approximately 92%) of GABA-induced currents, when tested at 500 μM using a patch-clamp technique. The second most active analogue was the 2-naphthyl analogue with approximately 85% inhibition. The 3-thienyl analogue demonstrated competitive inhibition of cockroach GABA receptors. Homology modeling and ligand docking studies predicted that hydrophobic 3-substituents could interact with an accessory binding site at the orthosteric binding site.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 19, 1 October 2012, Pages 5957-5964
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 19, 1 October 2012, Pages 5957-5964
نویسندگان
Mohammad Mostafizur Rahman, Yuki Akiyoshi, Shogo Furutani, Kazuhiko Matsuda, Kenjiro Furuta, Izumi Ikeda, Yoshihisa Ozoe,