| Identification | Back Directory | [Name]
1H-Indole-1-carboxamide, 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)- | [CAS]
200940-22-3 | [Synonyms]
SB 243213
1H-Indole-1-carboxamide, 2,3-dihydro-5-methyl-N-[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-6-(trifluoromethyl)- | [Molecular Formula]
C22H19F3N4O2 | [MOL File]
200940-22-3.mol | [Molecular Weight]
428.41 |
| Hazard Information | Back Directory | [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]
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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| [IC 50]
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) | [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 |
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