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 2.08uM.
Solubility:H2O
Primary Target:5-HT2C
Storage and Stability:Lyophilized powder may be stored at -20°C. Stable for 12 months at -20°C. Reconstitute with sterile buffer or dH2O. Aliquot to avoid repeated freezing and thawing. Store at -20°C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
