Recent developments in adenosine receptor ligands and their potential as novel drugs.
Recent developments in adenosine receptor ligands and their potential as novel drugs.
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DOI：
10.1016/j.bbamem.2010.12.017
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发表时间：
2011-05
影响因子：
3.4
通讯作者：
Jacobson, Kenneth A.
中科院分区：
文献类型：
--
作者：
Mueller, Christa E.;Jacobson, Kenneth A.
药物化学方法已应用于所有四种腺苷受体（AR）亚型（A1, A2A， A2B和A3），以创建每种受体的选择性激动剂和拮抗剂。最近报道的一类选择性AR配体是A2BAR激动剂。这些选择性配体的可用性促进了调节ar的治疗应用研究，并在某些情况下提供了临床候选药物。前药方法已经开发出来，可以提高药物的生物利用度，减少副作用，和/或可能导致位点选择性作用。A2A激动剂regadenoson （Lexiscan®）是一种心肌灌注成像诊断药物，是首个获批的选择性AR激动剂。其他选择性激动剂和拮抗剂正在或正在进行广泛适应症的临床试验，包括分别用于房颤或阵发性室上性心动过速的capadenoson和tecadenoson （A1激动剂），分别用于心肌灌注成像的apadenoson和binodenoson （A2A激动剂），用于治疗帕金森病的preladenant （A2A拮抗剂），以及分别用于炎症性疾病和癌症的CF101和CF102 （A3激动剂）。这篇文章是题为“腺苷受体”的特刊的一部分。
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”.
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影响因子：
3.6
作者：
Bilkei-Gorzo, Andras;Abo-Salem, Osama M.;Zimmer, Andreas
通讯作者：
Zimmer, Andreas
影响因子：
--
作者：
Borea, P A;Gessi, S;Fishman, P
通讯作者：
Fishman, P
影响因子：
3.5
作者：
Baraldi, Pier Giovanni;Tabrizi, Mojgan Aghazadeh;Preti, Delia
通讯作者：
Preti, Delia
影响因子：
3.5
作者：
Bertarelli, Daniela C G;Diekmann, Martina;Hayallah, Alaa M;Rusing, Dorothee;Iqbal, Jamshed;Preiss, Birgit;Verspohl, Eugen J;Muller, Christa E
通讯作者：
Muller, Christa E
DOI：
10.1124/jpet.108.148270
发表时间：
2009-04-01
影响因子：
3.5
作者：
Auchampach, John A.;Kreckler, Laura M.;Maas, Garren E.
通讯作者：
Maas, Garren E.