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[1].
ChEBI: SB 243213 is an indolyl carboxylic acid.
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].
| Animal Model: | Male Sprague-Dawley experimentally naive rats (220-300 g)[1] |
| 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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Human 5-HT2C Receptor: 9.37 (pKi); human 5-HT1A Receptor: <5.3 (pKi); human 5-HT1B Receptor: 5.5 (pKi); human 5-HT1D Receptor: 6.32 (pKi); human 5-HT1E Receptor: <5.4 (pKi); 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)
[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. DOI:
10.1016/s0028-3908(01)00054-5
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