SB 243213 hydrochloride is an orally active, selective and high-affinity 5-hydroxytryptamine (5-HT)_2C receptor antagonist with a pK_i of 9.37 and a pK_b of 9.8 for human 5-HT_2C receptor. SB 243213 hydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders^[1]. In Vitro: SB 243213 hydrochloride showed little affinity (pK_i<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It showed weak affinity (pK_i<6.5) for the cloned human 5-HT1D and D3 receptors and moderate affinity (pK_i=6.7) for the cloned human D2 receptor^[1].
In Vivo: SB 243213 hydrochloride (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box^[1].
SB 243213 hydrochloride (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction^[1].