New, Non-Adenosine, High-Potency Agonists for the Human Adenosine A_2B Receptor with an Improved Selectivity Profile Compared to the Reference Agonist N-Ethylcarboxamidoadenosine

Citations Over TimeTop 10% of 2004 papers

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.

Related Papers

• → New, Non-Adenosine, High-Potency Agonists for the Human Adenosine A_2B Receptor with an Improved Selectivity Profile Compared to the Reference Agonist N-Ethylcarboxamidoadenosine(2004)150 cited
• → 2,8-Disubstituted adenosine derivatives as partial agonists for the adenosine A2A receptor(2003)31 cited
• → Adenosine receptors involved in modulation of noradrenaline release in isolated rat tail artery(2004)21 cited
• → Prolonged in vitro exposure of rat brain slices to adenosine analogues: Selective desensitization of adenosine A1 but not A2 receptors(1992)61 cited
• [The comparative characteristics and receptor mechanism of the effect of adenosine-receptor agonists in total cerebral ischemia].(1994)