General description
A selective, brain-penetrant 5-HT2C receptor antagonist (pKi 8.2-9.0 ), with some effects on the 5-HT2B receptor (pKi 6.8-7.0) and 5-HT2A receptor (pKi 6.1-6.8). SB 242084 has been shown to increase the effectiveness of the selective serotonin reuptake inhibitor (SSRI) class of antidepressants, and may also reduce their side effects. In animal studies, SB-242,084 produced stimulant-type activity and reinforcing effects, somewhat similar to but much weaker than cocaine or amphetamines. In vivo (ocular) IC50 values reported at 2.08 µM.
Biochem/physiol Actions
Primary Target
5-HT2C
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Manvich, D. F., et al. 2012. J Pharmacol. Exp. Ther.342, 761.
Burghardt, N. S., et al. 2007. Biol Psychiatry62, 1111.
Sharif, N. A., et al. 2007. J. Ocul. Pharmacol. Ther.23, 1.
Knight A. R., et al. 2004. Naunyn Schmiedebergs Arch. Pharmacol.370, 114.
Kennett G.A., et al. 1997. Neuropharmacol. 36, 609.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥98% (HPLC) |
| Quality Segment | 100 |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white to pale yellow,pale yellow |
| solubility | water: soluble |
| storage temp. | −20°C |
| SMILES string | Clc1cc2c(cc1C)CCN2C(=O)Nc3cnc(cc3)Oc4c(nccc4)C.Cl.Cl |
| InChI | 1S/C21H19ClN4O2.2ClH/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2;;/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27);2*1H |
| InChI key | GCMNSEILNIPNSX-UHFFFAOYSA-N |
