The discovery of a selective, high affinity A2B adenosine receptor antagonist for the potential treatment of asthma

doi:10.1016/j.bmcl.2004.11.044

Bioorganic & Medicinal Chemistry Letters

Volume 15, Issue 3, 1 February 2005, Pages 609-612

https://doi.org/10.1016/j.bmcl.2004.11.044 Get rights and content

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 A₁ > 200: A_2A > 200: A₃ > 167).

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Acknowledgements

We would like to thank Dr. Brent Blackburn, and Dr. Luiz Belardinelli, for valuable input and discussion. The authors would like to thank Yuzhi Wu and Marie Nguyen for technical help.

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The discovery of a selective, high affinity A2B adenosine receptor antagonist for the potential treatment of asthma

Abstract

Graphical abstract

Section snippets

Acknowledgements

Ann. Emerg. Med.

Bioorg. Med. Chem. Lett.

Pharmacol. Rev.

J. Immunol.

Am. J. Respir. Cell Mol. Biol.

Allergy Asthma Proc.

Pediatr. Emerg. Care

The discovery of a selective, high affinity A_2B adenosine receptor antagonist for the potential treatment of asthma