期刊
CURRENT TOPICS IN MEDICINAL CHEMISTRY
卷 10, 期 9, 页码 878-901出版社
BENTHAM SCIENCE PUBL LTD
DOI: 10.2174/156802610791268729
关键词
Adenosine; A(1) receptor; agonists; antagonists; SAR; heterocyclic compounds
资金
- Italian MIUR [2008]
- University of Genoa
Adenosine is a neuromodulator that interacting with four receptors, A(1), A(2A), A(2B) and A(3), is involved in the regulation of several biological functions in different organs and tissues, including the central nervous system, the cardiovascular system and the airways; many pathophysiological states are associated with changes of adenosine levels. For these reasons pharmaceutical companies and academicians performed intense efforts to obtain agonists, antagonists and allosteric enhancers selective for each adenosine receptor subtypes as potential clinical candidates. In fact, therapeutic modulation of the adenosine system could offer the possibility of a soft treatment of different diseases, but, due to the ubiquitous distribution of adenosine and of its receptors, the challenge in therapy development depends from specificity for the different receptor subtypes. Some A(1) agonists and antagonists, very potent and selective, reached clinical trials for the treatment of different diseases. A(1) agonists are clinical candidates for atrial arrhythmias, angina, type 2 diabetes and in pain management, while A(1) antagonists are in study as potassium-sparing diuretics with kidney-protecting properties and in chronic heart diseases. Several reviews, recently published and herein cited, reported in detail the biological and clinical aspects of such molecules. This review focuses on the A(1) adenosine receptor (A(1)AR) ligands, both agonists and antagonists, appeared in the literature in the last few years, together with their potential therapeutic application, pointing the attention on their chemical structures and SAR (Structure Activity Relationship) and also reporting new findings on preclinical or clinical trials of some important A(1)AR ligands synthesized in the past.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据