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Biological Activity:
Potent and selective adenosine A1 receptor antagonist, with Ki values to be 0.19 nM and 170 nM for A1 and A2 receptors resepectively.
References: online
H Nonaka et al. KW-3902, a selective high affinity antagonist for adenosine A1 receptors. Br J Pharmacol. 1996, 117(8), 1645–1652. [online]
MM Givertz et al. The effects of KW-3902, an adenosine A1-receptor antagonist, on diuresis and renal function in patients with acute decompensated heart failure and renal impairment or diuretic resistance. J. Am. Coll. Cardiol. 2007, 50(16), 1551–60.
BM Massie et al. Rolofylline, an Adenosine A1−Receptor Antagonist, in Acute Heart Failure. N. Engl. J. Med. 2010, 363(15), 1419-28.
Chemical Name: 8-(Hexahydro-2,5-methanopentalen-3a(1H)-yl)-3,7-dihydro-1,3-dipropyl-1H-purine-2,6-dione |