Current status of A1 adenosine receptor allosteric enhancers

被引：0
作者：
Romagnoli, Romeo [1 ]
Baraldi, Pier Giovanni [1 ]
Moorman, Allan R. [2 ]
Borea, Pier Andrea [3 ]
Varani, Katia [3 ]
机构：
[1] Univ Ferrara, Dipartimento Sci Chim & Farmaceut, I-44121 Ferrara, Italy
[2] Alta Vetta Pharmaceut Consulting LLC, Durham, NC USA
[3] Univ Ferrara, Dipartimento Sci Med, Sez Farmacol, I-44121 Ferrara, Italy
来源：
FUTURE MEDICINAL CHEMISTRY | 2015年 / 7卷 / 10期
关键词：
2ND EXTRACELLULAR LOOP; BIOLOGICAL EVALUATION; ADENOSINE-A1-RECEPTOR BINDING; INTERNATIONAL UNION; MODULATION; 2-AMINO-3-BENZOYLTHIOPHENES; NOMENCLATURE; PHARMACOLOGY; DERIVATIVES; ACTIVATION;
D O I：
10.4155/FMC.15.65
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Adenosine is an ubiquitous nucleoside involved in various physiological and pathological functions by stimulating A(1), A(2A), A(2B) and A(3) adenosine receptors (ARs). Allosteric enhancers to A(1)ARs may represent novel therapeutic agents because they increase the activity of these receptors by mediating a shift to their active form in the A(1)AR-G protein ternary complex. In this manner, they are able to amplify the action of endogenous adenosine, which is produced in high concentrations under conditions of metabolic stress. A(1)AR allosteric enhancers could be used as a justifiable alternative to the exogenous agonists that are characterized by receptor desensitization and downregulation. In this review, an analysis of some of the most interesting allosteric modulators of A(1)ARs has been reported.
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收藏
页码：1247 / 1259
页数：13
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