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New, Non-Adenosine, High-Potency Agonists for the Human Adenosine A2B Receptor With an Improved Selectivity Profile Compared to the Reference Agonist N-ethylcarboxamidoadenosine

New, Non-Adenosine, High-Potency Agonists for the Human Adenosine A2B Receptor With an Improved Selectivity Profile Compared to the Reference Agonist N-ethylcarboxamidoadenosine

Margot W Beukers, Lisa C W Chang, Jacobien K von Frijtag Drabbe Künzel, Thea Mulder-Krieger, Ronald F Spanjersberg, Johannes Brussee, Ad P IJzerman

J Med Chem. 2004 Jul 15;47(15):3707-9.

PMID: 15239649

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.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP333962917	LUF5834		333962-91-7	Price

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