Biochem/physiol Actions

Primary Target5-HT_2C

General description

A selective, brain-penetrant 5-HT_2C receptor antagonist (pKi 8.2-9.0 ), with some effects on the 5-HT_2B receptor (pKi 6.8-7.0) and 5-HT_2A 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Other Notes

Manvich, D. F., et al. 2012. J Pharmacol. Exp. Ther.342, 761.Burghardt, N. S., et al. 2007. Biol Psychiatry62, 1111.r>Sharif, N. A., et al. 2007. J. Ocul. Pharmacol. Ther.23, 1. r>Knight A. R., et al. 2004. Naunyn Schmiedebergs Arch. Pharmacol.370, 114.Kennett G.A., et al. 1997. Neuropharmacol. 36, 609.

Packaging

10 mg in Glass bottle

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)