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Table 1 Binding affinities calculated from radiologand ([125I]I-AB-MECA) binding experiments.

From: Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A3 adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts

Agonist

mA3AR,

Ki or Kiapp (nM)

mA1AR,

Ki or Kiapp (nM)

Selectivity (A1 /A3)

MRS5246

0.04 ± 0.002

14.35 ± 4.35

359-fold

MRS5233

3.94 ± 0.31

665 ± 70

169-fold

 

98.5-fold increase

(MRS5233/MRS5246)

46.3-fold increase

(MRS5233/MRS5246)

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