Adenosine receptor inhibitor 1 is a highly potent and selective antagonist of adenosine receptor (AR), exhibiting 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, holding great promise for investigating cancer and neurodegenerative diseases [1].

A2A receptor:68.5 nM (Ki), A3 receptor:>1000 nM (Ki), A1AR:>1000 nM (Ki), A2B (human):>1000 nM (Ki)

Compound 12d, an adenosine receptor inhibitor, demonstrates metabolic stability with 96.56% and 97.97% of the parent compound remaining after a 120-minute incubation with mouse liver microsomes (MLMs) and rat liver microsomes (RLMs), respectively [1].

Adenosine receptor inhibitor 1 administered intraperitoneally (i.p.) at doses of 20, 30, 40 mg/kg demonstrated concentration-dependent antinociceptive effects, reducing the pain response in animal models. Specifically, at a 20 mg/kg dose, it exhibited an anti-inflammatory effect, reducing edema in a carrageenan-induced model, and at doses of 5, 10, 20 mg/kg, it showed significant analgesic effects in mice, reducing pain from peripheral sources. In an 18-26 g male albino Swiss mouse model with chronic pain induced by 5% formalin, doses of 20, 30, 40 mg/kg decreased the licking/biting time of the irritated paw. In 150-180 g male Wistar rats experiencing carrageenan-induced edema, a 20 mg/kg dose inhibited edema by 23.3%, 54.2%, and 66.0% over 1, 2, and 3 hours, respectively. Furthermore, in mice injected with irritants such as phenylbenzoquinone or acetic acid to induce pain, doses of 5, 10, 20 mg/kg led to a decrease in pain manifestations by 32.9%, 54.9%, and 82.0%, respectively.