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U-92016A is an agonist of the serotonin (5-HT) receptor subtype 5-HT1A (Ki = 0.4 nM). It is selective for 5-HT1A over 5-HT1D, 5-HT2, dopamine D1 and D2, and α1- and α2-adrenergic receptors (Kis = 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-HT1A. 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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