The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor.

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DeNinno MP, Masamune H, Chenard LK, DiRico KJ, Eller C, Etienne JB, Tickner JE, Kennedy SP, Knight DR, Kong J, Oleynek JJ, Tracey WR, Hill RJ

The synthesis of highly potent, selective, and water-soluble agonists at the human adenosine A3 receptor.

Bioorg Med Chem Lett. 2006 May 1;16(9):2525-7. Epub 2006 Feb 7.

PubMed ID

16464581 [ View in PubMed

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Abstract

Using a combination of parallel and directed synthesis, the discovery of a highly potent and selective series of adenosine A3 agonists was achieved. High aqueous solubility, required for the intended parenteral route of administration, was achieved by the presence of one or two basic amine functional groups.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Piclidenoson	Adenosine receptor A3	Ki (nM)	4.4	N/A	N/A	Details