FK-453

FK-453 is an adenosine A₁ receptor antagonist (K_i = 18 nM).¹ It is selective for the adenosine A₁ receptor over the adenosine A_2A and A₃ receptors (K_is = 1,300 and 2,800 nM, respectively). FK-453 reduces adenosine-induced negative inotropic activity in isolated guinea pig atrial strips (IC₅₀ = 560 pM).² It has diuretic activity in rats, where it increases urine volume and sodium excretion when administered at a dose of 10 mg/kg, and reduces cyclosporin-induced nephrotoxicity in rats at 100 mg/kg.^3,4

WARNING This product is not for human or veterinary use.

1. Harada, H., Asano, O., Hoshino, Y., et al. 2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: Their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A2B receptor. J. Med. Chem. 44(2), 170-179 (2001).

2. Terai, T., Kita, Y., Kusunoki, T., et al. A novel non-xanthine adenosine A₁ receptor antagonist. Eur. J. Pharmacol. 279(2-3), 217-225 (1995).

3. Balakrishnan, V.S., von Ruhland, C.J., Griffiths, D.F., et al. Effects of a selective adenosine A₁ receptor antagonist on the development of cyclosporin nephrotoxicity. Br. J. Pharmacol. 117(5), 879-884 (1996).

4. Akahane, A., Katayama, H., Mitsunaga, T., et al. Discovery of FK453, a novel non-xanthine adenosine A₁ receptor antagonist. Biooorg. Med. Chem. Lett. 6(17), 2059-2062 (1996).