Partial Agonists for A3 Adenosine Receptors
نویسندگان
چکیده
منابع مشابه
2-triazole-substituted adenosines: a new class of selective A3 adenosine receptor agonists, partial agonists, and antagonists.
"Click chemistry" was explored to synthesize two series of 2-(1,2,3-triazolyl)adenosine derivatives (1-14). Binding affinity at the human A(1), A(2A), and A(3)ARs (adenosine receptors) and relative efficacy at the A(3)AR were determined. Some triazol-1-yl analogues showed A(3)AR affinity in the low nanomolar range, a high ratio of A(3)/A(2A) selectivity, and a moderate-to-high A(3)/A(1) ratio. ...
متن کاملThe synthesis of a series of adenosine A3 receptor agonists.
A series of 1'-(6-aminopurin-9-yl)-1'-deoxy-N-methyl-β-d-ribofuranuronamides that were characterised by 2-dialkylamino-7-methyloxazolo[4,5-b]pyridin-5-ylmethyl substituents on N6 of interest for screening as selective adenosine A3 receptor agonists, have been synthesised. This work involved the synthesis of 2-dialkylamino-5-aminomethyl-7-methyloxazolo[4,5-b]pyridines and analogues that were cou...
متن کاملThe role of adenosine A3 receptors in cytotoxicity of the breast cancer cell lines
The nucleoside adenosine is present within cells and body fluids of all living organisms and its production, both intra- and extracellularly, is tightly coupled to energy consumption resulting in increased level of extracellular adenosine. The physiological effects of adenosine are mediated through four pharmacologically and biochemically distinct adenosine receptors (AR), i.e. A1, A2A, A2B and...
متن کاملKnockout of A3 adenosine receptors reduces mouse intraocular pressure.
PURPOSE To test the putative role of A(3) adenosine receptors (ARs) in modulating intraocular pressure (IOP). METHODS IOP was monitored for up to 32 minutes in A3-knockout (A3AR-/-) and A3AR+/+ control mice by the servo-null approach. The IOP responses to adenosine, A3AR agonists and A3AR antagonists were studied singly or in combination in both strains. RESULTS IOP was significantly lower ...
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Adenosine is a metabolite, which has long been implicated in a variety of inflammatory processes. Inhaled adenosine provokes bronchoconstriction in asthmatics or chronic obstructive pulmonary disease patients, but not in non-asthmatics. This hyper responsiveness to adenosine appears to be mediated by mast cell activation. These observations have marked the receptor that mediates the bronchocons...
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ژورنال
عنوان ژورنال: Current Topics in Medicinal Chemistry
سال: 2004
ISSN: 1568-0266
DOI: 10.2174/1568026043450989