Abstract
The adenosine A(2B) receptor is the least well characterized of the four known adenosine receptor subtypes because of the absence of potent, selective agonists. Here, we present five non-adenosine agonists. Among them, 2-amino-4-(4-hydroxyphenyl)-6-(1H-imidazol-2-ylmethylsulfanyl)pyridine-3,5-dicarbonitrile, 17, LUF5834, is a high-efficacy partial agonist with EC(50) = 12 nM and 45-fold selectivity over the adenosine A(3) receptor but lacking selectivity versus the A(1) and A(2A) subtypes. Compound 18, LUF5835, the 3-hydroxyphenyl analogue, is a full agonist with EC(50) = 10 nM.
MeSH terms
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Adenosine A2 Receptor Agonists*
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Adenosine-5'-(N-ethylcarboxamide) / chemistry
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Adenosine-5'-(N-ethylcarboxamide) / pharmacology*
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Aminopyridines / chemical synthesis*
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Aminopyridines / chemistry
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Aminopyridines / pharmacology
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Animals
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CHO Cells
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Cricetinae
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Cyclic AMP / biosynthesis
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / chemistry
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Imidazoles / pharmacology
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Structure-Activity Relationship
Substances
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2-amino-4-(4-hydroxyphenyl)-6-(1H-imidazol-2-ylmethylsulfanyl)pyridine-3,5-dicarbonitrile
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Adenosine A2 Receptor Agonists
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Aminopyridines
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Imidazoles
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Adenosine-5'-(N-ethylcarboxamide)
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Cyclic AMP