U-99194 (maleate)

U-99194 is a dopamine D₃ receptor antagonist (K_i = 160 nM for the human receptor).¹ It is selective for dopamine D₃ receptors over the α₁-adrenergic receptor (α₁-AR; K_i = 8,913 nM for the rat receptor), M₁ muscarinic acetylcholine receptor (mAChR), serotonin (5-HT) receptor subtype 5-HT_1A, and dopamine D₄ receptor (K_is = 2,090, 4,230, and >10,000 nM for the human receptors). U-99194 reverses hypothermia induced by the D₃ receptor agonists (+)-7-OH-DPAT or (+)-PD 128907 (Item No. 21235) in rats with half-maximal inhibitory dose (ID₅₀) values of 19.1 and 12.9 mg/kg, respectively. It increases non-social exploration, social investigation, and the latency to attack in a mouse model of isolation-induced aggressiveness when administered at a dose of 40 mg/kg.²

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1. Audinot, V., Newman-Tancredi, A., Gobert, A., et al. A comparative in vitro and in vivo pharmacological characterization of the novel dopamine D₃ receptor antagonists (+)-S 14297, nafadotride, GR 103,691 and U 99194. J. Pharmacol. Exp. Ther. 287(1), 187-197 (1998).

2. Rodríguez-Arias, M., Felip, C.M., Broseta, I., et al. The dopamine D₃ antagonist U-99194A maleate increases social behaviors of isolation-induced aggressive male mice. Psychopharmacology (Berl.) 144(1), 90-94 (1999).