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-HT 1A Receptor:0.2 nM (Ki)

U92016A (U-92016A) is selective for the 5-HT1A receptor over other biogenic amine receptors. U92016A decreases the Forskolin-induced increase in cyclic AMP synthesis and has an intrinsic activity of 0.82 relative to 5-HT in Chinese hamster ovary cells expressing the human 5HT1A receptor [2].

U92016A (U-92016A) potently decreases rectal temperature in mice. U92016A also elicits the 5-HT-mediated syndrome in rats and results in a dose-related decrease in 5-hydroxytryptophan accumulation. U92016A also decreases arterial blood pressure in spontaneously hypertensive rats and inhibits sympathetic nerve activity in cats. U92016A displays excellent potency and a long duration of action. U92016A also inhibits the firing of dorsal raphe 5-HT neurons and is active in two social interaction assays. The p.o. bioavailability of U92016A is 45% [2].