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,
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