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.
Uses
VUF 5574 is an adenosine A3 receptor antagonist.
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.
IC 50
Recombinant Human Adenosine A
3 receptor (A
3R): 4.03 nM (Ki)
References
[1] JACQUELINE E. VAN MUIJLWIJK-KOEZEN. Isoquinoline and Quinazoline Urea Analogues as Antagonists for the Human Adenosine A3 Receptor[J]. Journal of Medicinal Chemistry, 2000, 43 11: 2227-2238. DOI:
10.1021/jm000002u[2] JIANZHONG SHEN. Cell-signaling evidence for adenosine stimulation of coronary smooth muscle proliferation via the A1 adenosine receptor.[J]. Circulation research, 2005, 97 6: 574-582. DOI:
10.1161/01.res.0000181159.83588.4b[3] ANNA MARIA PUGLIESE. A3 adenosine receptor antagonists delay irreversible synaptic failure caused by oxygen and glucose deprivation in the rat CA1 hippocampus in vitro[J]. British Journal of Pharmacology, 2009, 147 5: 524-532. DOI:
10.1038/sj.bjp.0706646[4] MAHMOUD M. EL-MAS. Role of adenosine A2A receptor signaling in the nicotine-evoked attenuation of reflex cardiac sympathetic control[J]. Toxicology and applied pharmacology, 2011, 254 3: Pages 229-237. DOI:
10.1016/j.taap.2011.04.014
