ChemicalBook CAS DataBase List 200940-22-3

200940-22-3

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
Molecular Formula	C22H19F3N4O2
Molecular Weight	428.41
MOL File	200940-22-3.mol

Chemical Properties

storage temp.	Store at -20°C
form	Solid
color	White to off-white

Hazard Information

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.

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

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