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

…, R Kalla, T Perry, V Palle, V Varkhedkar, D Xiao…

文献索引：Zablocki, Jeff; Kalla, Rao; Perry, Thao; Palle, Venkata; Varkhedkar, Vaibhav; Xiao, Dengming; Piscopio, Anthony; Maa, Tenning; Gimbel, Art; Hao, Jia; Chu, Nancy; Leung, Kwan; Zeng, Dewan Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 3 p. 609 - 612

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被引用次数: 53

摘要

Adenosine has been suggested to play a role in asthma, possibly via activation of A2B adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A2B AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A2B AdoR antagonist with good selectivity (A2B AdoR Ki= 50nM, selectivity A1> 200: A2A> 200: A3> 167).