The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.

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Zablocki J, Kalla R, Perry T, Palle V, Varkhedkar V, Xiao D, Piscopio A, Maa T, Gimbel A, Hao J, Chu N, Leung K, Zeng D

The discovery of a selective, high affinity A(2B) adenosine receptor antagonist for the potential treatment of asthma.

Bioorg Med Chem Lett. 2005 Feb 1;15(3):609-12.

PubMed ID

15664822 [ View in PubMed

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Abstract

Adenosine has been suggested to play a role in asthma, possibly via activation of A(2B) adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A(2B) AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A(2B) AdoR antagonist with good selectivity (A(2B) AdoR K(i)=50 nM, selectivity A(1)>200: A(2A)>200: A(3)>167).

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Theophylline	Adenosine receptor A1	Ki (nM)	0.6	N/A	N/A	Details
Theophylline	Adenosine receptor A2a	Ki (nM)	0.6	N/A	N/A	Details
Theophylline	Adenosine receptor A2b	Ki (nM)	7059	N/A	N/A	Details