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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.
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.
数据表
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
1260505-34-7
Chemical formula
C₂₁H₁₉ClN₄O₂·HCl
Structure formula
Purity
≥98% by HPLC
Solubility
DMSO (50 mM) or H₂O (50 mM)
Storage
Protect from light
-20°C
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.