New, non-adenosine, high-potency agonists for the human adenosine A2B receptor with an improved selectivity profile compared to the reference agonist N-ethylcarboxamidoadenosine

Journal of Medicinal Chemistry
Margot W BeukersA P IJzerman

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.

References

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Citations

Apr 12, 2008·Purinergic Signalling·Stefania GessiPier Andrea Borea
Apr 30, 2008·Purinergic Signalling·Pier Giovanni BaraldiDelia Preti
Feb 3, 2009·Purinergic Signalling·Pier Giovanni BaraldiDelia Preti
Oct 12, 2012·Purinergic Signalling·Ellen V LangemeijerAd P Ijzerman
Jan 26, 2013·Chemical Reviews·Bagher Eftekhari-SisAli Akbari
Jan 26, 2010·Journal of Medicinal Chemistry·Vsevolod KatritchRuben Abagyan
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Jul 19, 2006·Medicinal Research Reviews·Margot W BeukersAdriaan P Ijzerman
Oct 11, 2019·Pharmaceuticals·Diego Dal BenRosaria Volpini
Feb 12, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Eszter SzennyesÉva Bokor
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