U-92016A

U-92016A is an agonist of the serotonin (5-HT) receptor subtype 5-HT_1A (K_i = 0.4 nM).¹ It is selective for 5-HT_1A over 5-HT_1D, 5-HT₂, dopamine D₁ and D₂, and α₁- and α₂-adrenergic receptors (K_is = 7.7, >1,000, >1,000, 36, >1,000, and >1,000 nM, respectively). U-92016A inhibits forskolin-stimulated cAMP synthesis in CHO cells transfected with human 5-HT_1A. In vivo, U-92016A induces hypothermia in mice (ED₅₀ = 0.041 mg/kg). It induces 5-HT syndrome, as measured by increased flat body posture and reciprocal forepaw treading, as well as decreases accumulation of 5-HT and dopamine in rats when administered at a dose of 5 mg/kg. U-92016A also decreases arterial blood pressure and heart rate in a dose-dependent manner in spontaneously hypertensive rats and reverses isolation-induced aggression in mice.

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1. McCall, R.B., Romero, A.G., Bienkowski, M.J., et al. Characterization of U-92016A as a selective, orally active, high intrinsic activity 5-hydroxytryptamine1A agonist. J. Pharmacol. Exp. Ther. 271(2), 875-883 (1994).