SB 243213 dihydrochloride is an orally active, selective and high-affinity5-HT_2Creceptorantagonist with apK_iof 9.37 and apK_bof 9.8 for human 5-HT_2Creceptor. SB 243213 dihydrochloride shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 dihydrochloride has improved anxiolytic profile and has the potential for schizophrenia and motor disorders^[1].

SB 243213 dihydrochloride shows little affinity (pK_i<6) for cloned human 5-HT_1A, 5-HT_1B, 5-HT_1E, 5- HT_1Fand 5-HT₇receptors. It shows weak affinity (pK_i<6.5) for the cloned human 5-HT_1Dand D3 receptors and moderate affinity (pK_i=6.7) for the cloned human D2 receptor^[1].
SB 243213 dihydrochloride shows 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels^[1].

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

501.33

Solid

C₂₂H₂₁Cl₂F₃N₄O₂

1780372-25-9

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)