SB 243213 

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^[1].

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^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

428.41

Solid

C₂₂H₁₉F₃N₄O₂

200940-22-3

O=C(N1CCC2=C1C=C(C(F)(F)F)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3

Room temperature in continental US; may vary elsewhere.

• [1]. Wood MD, et al. SB-243213; a selective 5-HT2C receptor inverse agonist with improved anxiolytic profile: lack of tolerance and withdrawal anxiety. Neuropharmacology. 2001 Aug;41(2):186-99.  [Content Brief]