کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584334 | 981329 | 2014 | 12 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Carbamazepine derivatives with P2X4 receptor-blocking activity
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کلمات کلیدی
inflammation - التهاب( توروم) Neuropathic pain - درد نوروپاتیکStructure–activity relationship - رابطه ساختار-فعالیتSynthesis - سنتزTricyclics - سه چرخهnegative allosteric modulator - منحنی آلوزیستریک منفیHeterocycles - هتروسیکلligand-gated ion channel - کانال یون لیگاند دارP2X4 receptor - گیرنده P2X4
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Antagonists for the P2 receptor subtype P2X4, an ATP-activated cation channel receptor, have potential as novel drugs for the treatment of neuropathic pain and other inflammatory diseases. In the present study, a series of 47 carbamazepine derivatives including 32 novel compounds were designed, synthesized, and evaluated as P2X4 receptor antagonists. Their potency to inhibit ATP-induced calcium influx in 1321N1 astrocytoma cells stably transfected with the human P2X4 receptor was determined. Additionally, species selectivity (human, rat, mouse) and receptor subtype selectivity (P2X4 vs P2X1, 2, 3, 7) were investigated for selected derivatives. The most potent compound of the present series, which exhibited an allosteric mechanism of P2X4 inhibition, was N,N-diisopropyl-5H-dibenz[b,f]azepine-5-carboxamide (34, IC50 of 3.44 μM). The present study extends the so far very limited knowledge on structure-activity relationships of P2X4 receptor antagonists.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 3, 1 February 2014, Pages 1077-1088
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 3, 1 February 2014, Pages 1077-1088
نویسندگان
Maoqun Tian, Aliaa Abdelrahman, Stephanie Weinhausen, Sonja Hinz, Stefanie Weyer, Stefan Dosa, Ali El-Tayeb, Christa E. Müller,