Adenosine A ₁ Receptor Antagonists at a Fork in the Road

Purinergic Signaling and Blood Vessels in Health and Disease

“…Juxtamedullary Afferent Arterioles. Afferent arteriolar A 1 receptors mediate constriction, whereas A 2 receptors on afferent and efferent arterioles mediate dilation (Murray and Churchill, 1985;Holz and Steinhausen, 1987;Givertz, 2009). Afferent arterioles perfused with adenosine responded with persistent vasoconstriction via A 1 receptors on the smooth muscle (Hansen and Schnermann, 2003;Hansen et al, 2007).…”

Cardiac purinergic signalling in health and disease

“…A1R antagonists improved glomerular filtration, but simultaneously promoted natriuresis and diuresis in patients with heart failure [466][467][468]. A1R antagonists have been recommended for the treatment of cardiorenal syndrome [469]. Therefore, A1R antagonists are not recommended as a treatment for acute heart failure with renal dysfunction [470,471], although rolofylline, a selective A1R antagonist, had some beneficial effects for high risk acute decompensated heart failure [472].…”

Xanthines as Adenosine Receptor Antagonists

“…Yet other applications are cardiac arrhythmia, asthma and other respiratory disorders, and the prevention of organ damage, e.g. resulting from transplantation (Jacobson et al 1992a; Müller et al 1996; Müller 1997; Jacobson et al 2006; Moro et al 2006; Givertz 2009). …”