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Description
Overview
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.
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.
Product Information
CAS number
181632-25-7
Form
Off-white to pale yellow solid
Hill Formula
C₂₁H₁₉ClN₄O₂·HCl
Chemical formula
C₂₁H₁₉ClN₄O₂·HCl
Structure formula Image
Applications
Biological Information
Primary Target
5-HT2C
Purity
≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code
Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
Toxicity
Standard Handling
Storage
-20°C
Protect from Light
Protect from light
Do not freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Packaging Information
Transport Information
Supplemental Information
Specifications
Documentation
SB 242084 Hydrochloride - CAS 181632-25-7 - Calbiochem SDS
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.
Data Sheet
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.
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.
Form
Off-white to pale yellow solid
CAS number
181632-25-7
Chemical formula
C₂₁H₁₉ClN₄O₂·HCl
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (50 mM) or H₂O (50 mM)
Storage
-20°C
Protect from light
Do Not Freeze
Ok to freeze
Special Instructions
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity
Standard Handling
References
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.
