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Description

An adenosine analog that acts as a selective, high affinity agonist for Adenosine A1 receptor (A1R) (Ki = 800 pM, 2.3 µ,M, 18.8 µ,M, and 42 nM for human A1, A2A, A2B, A3 respectively). Shown to be centrally active following systemic administration and exhibits anti-convulsive effects. Also reported to inhibit adenylate cyclase activity in rat fat cell membrane (IC50 = 33 nM). Diminishes respiratory rhythm, reduces heart rate, and enhances the activity of KATP channels. Reduces norepinephrine release by about 50% in untreated and pertussis toxin treated hearts.