tonapofylline

Tonapofylline is a synthetic small molecule that acts as a selective antagonist of the A1 adenosine receptor (Ki ≈ 7.4 nM for human A1). It was developed primarily for research and potential therapeutic use in heart failure and has also been studied in models of kidney injury and other conditions involving adenosine signaling modulation. Unlike non-selective methylxanthines such as theophylline, tonapofylline exhibits high selectivity for the A1 subtype of adenosine receptors, which are implicated in renal function and cardiovascular regulation[6][8][10]. Its mechanism involves blocking the action of endogenous adenosine at these receptors to modulate physiological responses such as diuresis and natriuresis.

Other names

Tonapofilinatonapofyllinum3-[4-(2,6-dioxo-1,3-dipropyl-7H-purin-8-yl)-1-bicyclo[2.2.2]octanyl]propanoic acid3-(4-(2,6-dioxo-1,3-dipropyl-7H-purin-8-yl)-1-bicyclo[2.2.2]octanyl)propanoic acid