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SB 243213 is an orally active, selective and high-affinity 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 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

SB 243213 shows little affinity (pK_i<6) for cloned human 5-HT_1A, 5-HT_1B, 5-HT_1E, 5- HT_1F and 5-HT₇ receptors. It shows weak affinity (pK_i<6.5) for the cloned human 5-HT_1D and D3 receptors and moderate affinity (pK_i=6.7) for the cloned human D2 receptor.

SB 243213 (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.
SB 243213 (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction.

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