SB 243213 dihydrochlorideSB 243213 dihydrochloride
MedChemExpress (MCE)
HY-103112A
1780372-25-9
99.0%
4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months
-20°C, 1 month (sealed storage, away from moisture)
Room temperature in continental US
may vary elsewhere.
SB 243213 dihydrochloride 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 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.
SB 243213 dihydrochloride shows little affinity (pKi1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows weak affinity (pKi1D and D3 receptors and moderate affinity (pKi=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].
Human 5-HT2C Receptor 9.37 (pKi) human 5-HT1A Receptor human 5-HT1B Receptor 5.5 (pKi) human 5-HT1D Receptor 6.32 (pKi) human 5-HT1E Receptor human 5-HT1F Receptor 5.35 (pKi) Human 5-HT2A Receptor 7.01 (pKi) human 5-HT2B Receptor 7.2 (pKi) Human 5-HT6 Receptor 6.5 (pKi) Human 5-HT7 Receptor 5.64 (pKi)
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[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]