Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR). It exhibits exceptional affinity for A1 AR, A2A AR, A2B AR, and A3 AR, with respective Ki values of >1000, 68.5, >1000, >1000 nM. This compound demonstrates notable antinociceptive, anti-inflammatory, and peripheral analgesic properties. Therefore, Adenosine receptor inhibitor 1 holds great promise for investigating cancer and neurodegenerative diseases [1].

Adenosine receptor inhibitor 1 (compound 12d) (120 min) shows metabolic stability incubated with with 96.56 and 97.97% of the parent compound remained in the reaction mixtures after incubation with mouse (MLMs) and rat liver microsomes (RLMs), respectively [1].

Adenosine receptor inhibitor 1 (20, 30, 40 mg/kg; i.p.) shows antinociceptive activity at a concentration-dependent mannner [1]. Adenosine receptor inhibitor 1 (20 mg/kg; i.p.) shows anti-inflammatory effect in carrageenan-induced edema model [1]. Adenosine receptor inhibitor 1 (5, 10, 20 mg/kg; i.p.) shows analgesic effect in mouse [1]. Animal Model: 18-26 g male albino Swiss mice (chronic pain induced by the administration of 5% formalin) [1] Dosage: 20, 30, 40 mg/kg Administration: I.p. Result: Showed antinociceptive activity with decreasesed the licking/biting time of the right hind paw of mice in response to the irritating chemical stimulus. Animal Model: 150-180 g male rats Wistar(carrageenan-induced edema model) [1] Dosage: 20 mg/kg Administration: I.p. Result: Showed anti-inflammatory effect with the inhibition of 23.3%, 54.2%, 66.0% at 1h, 2h, 3h, respectively. Animal Model: Mouse (induce pain of peripheral origin by injection of an irritant like phenylbenzoquinone or acetic acid in mice) [1] Dosage: 5, 10, 20 mg/kg Administration: I.p. Result: Showed peripheral analgesic effect with the significant decrease in the number of writhings by 32.9%, 54.9%, 82.0% at doses of 5, 10, 20 mg/kg, respectively.