Description
VUF 5574 is an antagonist of the adenosine A
3 receptor (K
i = 4.03 nM for the recombinant human receptor). It is greater than 2,500-fold selective for adenosine A
3 over A
1 and A
2A receptors. VUF 5574 (100 nM) decreases phosphorylation of ERK1/2 induced by adenosine in isolated porcine coronary artery smooth muscle cells. It increases oxygen-glucose deprivation-induced reductions in the amplitude of field excitatory postsynaptic potentials (EPSPs) in a rat hippocampal slice model of ischemia when used at a concentration of 100 nM. VUF 5574 (2 μg, intracisternal) reduces sodium nitroprusside-induced heart rate increases in rats.
Biological Activity
Potent, selective, competitive antagonist for the human adenosine A 3 receptor (K i = 4 nM). Displays ≥ 2500-fold selectivity over A 1 and A 2A receptors.
