| Identification | Back 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 Properties | Back 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 |
| Hazard Information | Back 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.
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| 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.
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| [IC 50]
5-HT2A Receptor: 6.4 (pKi); 5-HT2B Receptor: 7.9 (pKi); 5-HT2C Receptor: 8.6 (pKi) |
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| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|