SB 242084 Selective 5-HT2C antagonist; brain penetrant

Chemical Name: 6-Chloro-2,3-dihydro-5-methyl-N-[6-­[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]-1H-indole­-1-carboxyamide dihydrochloride

Biological Activity
5-HT2C receptor antagonist that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively. Also displays selectivity orange of other 5-HT, dopamine and adrenergic receptors. Brain penetrant; exerts anxiolytic-like activity.ver a 

Technical Data
M.Wt:467.78
Formula:C21H19ClN4O2.2HCl
Solubility:Soluble to 50 mM in DMSO
Purity:>99 %
Storage:Desiccate at +4°C
CAS No:1215566-78-1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

References
Bromidge et al (1997) 6-Chloro-5-methyl-1-[[(2-methyl-3-pyridyl)oxy]-5-pyridyl]carbamoyl]-indoline (SB-242084): the first selective and brain penetrant 5-HT2C receptor antagonist. J.Med.Chem. 40 3494. PMID: 9357513.

Kennet et al (1997) SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology 36 609. PMID: 9225286.

Dalton et al (2006) Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse. Psychopharmacology 185 45. PMID: 16470405.