Tonapofylline (BG 9928) 是一种具有口服活性和选择性 A1 腺苷受体拮抗剂，对人 A1 腺苷受体 (hA1) 的 Ki 为 7.4 nM，选择性高出 A2A 腺苷受体 915 倍，A2B 腺苷受体 12 倍，正在开发为治疗心力衰竭的药物。
Tonapofylline (BG 9928) is an orally active and selective adenosine A1 receptor antagonist with a Ki of 7.4 nM for human adenosine A1 receptor (hA1), which displays 915-fold selectivity versus human adenosine A2A receptor and 12-fold selectivity versus human adenosine A2B receptor and is used in development for the treatment of heart failure[1][2]. Ki: 7.4 nM (Human adenosine A1 receptor)[1]
Tonapofylline (BG 9928) (1 mg/kg; p.o., b.i.d, days 0-6) produces sustained reductions in post-Cisplatin serum creatinine and blood urea nitrogen levels, improves body weight recovery and significant attenuation of Cisplatin-induced (5.5 mg/kg) kidney pathology scores[3]. Animal Model: Female viral antigen-free Sprague-Dawley rats[3]
[1]. Kiesman WF, et al. Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31. [2]. Ensor CR, et al. Tonapofylline: a selective adenosine-1 receptor antagonist for the treatment of heart failure. Expert Opin Pharmacother. 2010 Oct;11(14):2405-15. [3]. Gill A, et al. Protective effect of tonapofylline (BG9928), an adenosine A1 receptor antagonist, against cisplatin-induced acute kidney injury in rats. Am J Nephrol. 2009;30(6):521-6.
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