کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1944572 1053226 2011 19 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Recent developments in adenosine receptor ligands and their potential as novel drugs
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شیمی
پیش نمایش صفحه اول مقاله
Recent developments in adenosine receptor ligands and their potential as novel drugs
چکیده انگلیسی

Medicinal chemical approaches have been applied to all four of the adenosine receptor (AR) subtypes (A1, A2A, A2B, and A3) to create selective agonists and antagonists for each. The most recent class of selective AR ligands to be reported is the class of A2BAR agonists. The availability of these selective ligands has facilitated research on therapeutic applications of modulating the ARs and in some cases has provided clinical candidates. Prodrug approaches have been developed which improve the bioavailability of the drugs, reduce side-effects, and/or may lead to site-selective effects. The A2A agonist regadenoson (Lexiscan®), a diagnostic drug for myocardial perfusion imaging, is the first selective AR agonist to be approved. Other selective agonists and antagonists are or were undergoing clinical trials for a broad range of indications, including capadenoson and tecadenoson (A1 agonists) for atrial fibrillation, or paroxysmal supraventricular tachycardia, respectively, apadenoson and binodenoson (A2A agonists) for myocardial perfusion imaging, preladenant (A2A antagonist) for the treatment of Parkinson's disease, and CF101 and CF102 (A3 agonists) for inflammatory diseases and cancer, respectively. This article is part of a Special Issue entitled: “Adenosine Receptors”.

Research Highlights
► Potent, selective agonists and antagonists for all four AR subtypes have been developed.
► Prodrug approaches may lead to improved bioavailability.
► Regadenoson, an A2A-selective agonist was approved for myocardial perfusion imaging.
► Several adenosine receptor agonists and antagonists are currently evaluated in clinical trials.
► AR ligands are developed for CV, neurodegenerative and inflammatory diseases and cancer.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochimica et Biophysica Acta (BBA) - Biomembranes - Volume 1808, Issue 5, May 2011, Pages 1290–1308
نویسندگان
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