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196965-14-7

196965-14-7 Structure

196965-14-7 Structure
IdentificationBack Directory
[Name]

SB 221284
[CAS]

196965-14-7
[Synonyms]

SB 221284
5-(METHYLTHIO)-1-(3-PYRIDYLCARBAMOYL)-6-(TRIFLUOROMETHYL)INDOLINE
2,3-DIHYDRO-5-(METHYLTHIO)-N-3-PYRIDINYL-6-(TRIFLUOROMETHYL)-1H-INDOLE-1-CARBOXAMIDE
1H-Indole-1-carboxamide, 2,3-dihydro-5-(methylthio)-N-3-pyridinyl-6-(trifluoromethyl)-
[Molecular Formula]

C16H14F3N3OS
[MOL File]

196965-14-7.mol
[Molecular Weight]

353.36
Chemical PropertiesBack Directory
[Melting point ]

262-264 °C
[Boiling point ]

536.2±50.0 °C(Predicted)
[density ]

1.43±0.1 g/cm3(Predicted)
[storage temp. ]

Store at +4°C
[solubility ]

DMSO: ~14 mg/mL, soluble
[form ]

solid
[pka]

13.13±0.20(Predicted)
[color ]

white
Safety DataBack Directory
[WGK Germany ]

3
Hazard InformationBack Directory
[Uses]

SB 221284 is a potent, selective SR-2C/SR-2B antagonist.
[Definition]

ChEBI: SB 221284 is an indolyl carboxylic acid.
[Biological Activity]

Potent, selective 5-HT 2C/2B receptor antagonist. pK i values are 6.4, 7.9 and 8.6 for 5-HT 2A , 2B and 2C receptors respectively. Centrally active upon systemic administration in vivo .
[in vivo]

SB 221284 (0.1~1 mg/kg, i.p.) pre-treatment doses shows to block mCPP induced hypolocomotion, significantly enhances the hyperactivity induced by phencyclidine or MK-801[1].
SB 221284 (1 mg/kg, i.p.) significantly enhances the magnitude and duration of the increase induced by phencyclidine[1]

Animal Model:Male Sprague Dawley rats (250–360 g)[1]
Dosage:0.1~1 mg/kg
Administration:I.p.
Result:Pre-treatment doses showed to block mCPP induced hypolocomotion, significantly enhanced the hyperactivity induced by phencyclidine or MK-801.
Animal Model:Male Sprague Dawley rats (250–360 g)[1]
Dosage:1 mg/kg
Administration:I.p.
Result:Significantly enhanced the magnitude and duration of the increase induced by phencyclidine.
[IC 50]

5-HT2A Receptor: 6.4 (pKi); 5-HT2B Receptor: 7.9 (pKi); 5-HT2C Receptor: 8.6 (pKi)
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