U92016A hydrochloride is a potent and orally acitive agonist of 5-HT1A receptor which is metabolically stable. U92016A hydrochloride has an exceptionally high degree of intrinsic activity that binds with high affinity to human 5-HT1A receptors expressed in Chinese hamster ovary cells with Ki value of 0.2 nM [1] [2].

5-HT1A receptor:0.2 nM (Ki)

U92016A (U-92016A) exhibits selectivity toward the 5-HT1A receptor compared to other biogenic amine receptors. It reduces the increase in cyclic AMP synthesis induced by Forskolin and possesses an intrinsic activity of 0.82, relative to 5-HT, in Chinese hamster ovary cells that express the human 5HT1A receptor [2].

U92016A (U-92016A) significantly reduces rectal temperature in mice and induces a 5-HT-mediated syndrome in rats, accompanied by a dose-dependent reduction in 5-hydroxytryptophan accumulation. Additionally, it lowers arterial blood pressure in spontaneously hypertensive rats and suppresses sympathetic nerve activity in cats. Demonstrating strong efficacy and prolonged action, U92016A also inhibits the activity of dorsal raphe 5-HT neurons and proves effective in two social interaction assays, with an oral (p.o.) bioavailability of 45% [2].