SB 243213

Research use only, not for human use.

SB 243213 is an orally available and selective 5-HT2C receptor antagonist.SB 243213 has anxiolytic and antidepressant activity and is used in schizophrenia and movement disorders.

SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C 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 (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows weak affinity (pKi<6.5) for the cloned human 5-HT1D and D3 receptors and moderate affinity (pKi=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. 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.

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GPCR/G Protein

5-HT Receptor

5-HT Receptor

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200940-22-3

428.41

C22H19F3N4O2

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (291.78 mM; Ultrasonic )

Cc1cc2CCN(C(=O)Nc3ccc(Oc4cccnc4C)nc3)c2cc1C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years