Derenofylline

Derenofylline is an adenosine A₁ receptor antagonist (K_i = 1 nM).¹ It is selective for adenosine A₁ over A_2A, A_2B, and A₃ receptors (K_is = 398, 3,981, and 200 nM, respectively). It decreases adenosine A₁ receptor-mediated adenosine-induced bradycardia in rats (ED₅₀ = 0.49 mg/kg) but reduces A₂ receptor-mediated adenosine-induced hypotension by only 44.6% when administered at an intravenous dose of 5 mg/kg. It prevents increases in heart levels of collagen I and III in nephrectomized rats when administered at a dose of 10 mg/kg per day. Derenofylline also reduces relative plaque counts in a Zika virus plaque-forming assay in A549 cells (IC₅₀ = 58.6 nM) in an adenosine A₁ receptor-independent manner without inducing cytotoxicity when used at concentrations less than 10 µM.²

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1. Kalk, P., Eggert, B., Relle, K., et al. The adenosine A₁ receptor antagonist SLV320 reduces myocardial fibrosis in rats with 5/6 nephrectomy without affecting blood pressure. Br. J. Pharmacol. 151(7), 1025-1032 (2007).

2. Micewicz, E.D., Khachatoorian, R., French, S.W., et al. Identification of novel small-molecule inhibitors of Zika virus infection. Bioor. Med. Chem. Lett. 28(3), 452-458 (2018).