N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.

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Zhu R, Frazier CR, Linden J, Macdonald TL

N6-ethyl-2-alkynyl NECAs, selective human A3 adenosine receptor agonists.

Bioorg Med Chem Lett. 2006 May 1;16(9):2416-8. Epub 2006 Feb 17.

PubMed ID

16487705 [ View in PubMed

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Abstract

A series of N6-ethyl-2-alkynyl NECA (5'-N-ethylcarboxamidoadenosine) analogs were synthesized and their binding affinity with the four human adenosine receptors was evaluated. One of the compounds ZR1121 shows high affinity with hA3 receptor and its selectivity over hA1 receptor is 1-2 log orders greater than IB-MECA or Cl-IB-MECA, the currently employed selective A3 agonists.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Piclidenoson	Adenosine receptor A3	Ki (nM)	0.215	N/A	N/A	Details