5.06417

SB 242084 Hydrochloride

• Synonym(s): SB 242084 Hydrochloride, 5-HT _2C receptor antagonist, SB 242084 Hydrochloride, SB-242084 Hydrochloride, SB242084 Hydrochloride
• Empirical Formula (Hill Notation): C₂₁H₁₉ClN₄O₂ · xHCl
• CAS Number: 1260505-34-7
• Molecular Weight: 394.85 (free base basis)
• UNSPSC Code: 12352200

Properties

• Assay: ≥98% (HPLC)
• Quality Level: 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
• 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

Description

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.

Biochem/physiol Actions

Primary Target
5-HT_2C

Warning

Toxicity: Standard Handling (A)

Reconstitution

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

Safety Information

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point(F): Not applicable
• Flash Point(C): Not applicable