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, e
Storage Temp
Store at -20°C
Shipped In
Ice chest + Ice pads
Product Description
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
In Vitro
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-HT 7 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley experimentally naive rats (220-300 g) Dosage: 0.1, 0.3, 1, 3, 10 mg/kg Administration: PO; 1 hour pre-test Result: Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.
Form:Solid
IC50& Target:Human 5-HT 2C Receptor 9.37 (pKi) human 5-HT 1A Receptor <5.3 (pKi) human 5-HT 1B Receptor 5.5 (pKi) human 5-HT 1D Receptor 6.32 (pKi) human 5-HT 1E Receptor <5.4 (pKi) human 5-HT 1F Receptor 5.35 (pKi) Human 5-HT 2A Receptor 7.01 (pKi) human 5-HT 2B Receptor 7.2 (pKi) Human 5-HT 6 Receptor 6.5 (pKi) Human 5-HT 7 Receptor 5.64 (pKi)
