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

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

Author information

1
Division of Medicinal Chemistry, LACDR, Gorlaeus Laboratories, P.O. Box 9502, 2300 RA Leiden, The Netherlands. beukers@chem.leidenuniv.nl

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.

PMID:
15239649
DOI:
10.1021/jm049947s
[Indexed for MEDLINE]

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