1H-Indole-1-carboxamide, 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)-

Uses

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].

Definition

ChEBI: SB 243213 is an indolyl carboxylic acid.

in vivo

IC 50

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-HT₆ Receptor: 6.5 (pKi); Human 5-HT₇ Receptor: 5.64 (pKi)

References

[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