5.06417
SB 242084 Hydrochloride
≥98% (HPLC), 5-HT2C receptor antagonist, solid
别名:
SB 242084 Hydrochloride, 5-HT 2C receptor antagonist, SB 242084 Hydrochloride, SB-242084 Hydrochloride, SB242084 Hydrochloride
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关于此项目
经验公式（希尔记法）:
C21H19ClN4O2 · xHCl
化学文摘社编号:
分子量:
394.85 (free base basis)
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
产品名称
SB 242084 Hydrochloride,
SMILES string
Clc1cc2c(cc1C)CCN2C(=O)Nc3cnc(cc3)Oc4c(nccc4)C.Cl.Cl
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
assay
≥98% (HPLC)
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
Quality Level
Biochem/physiol Actions
Primary Target
5-HT2C
5-HT2C
Disclaimer
Toxicity: Standard Handling (A)
General description
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.
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.
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.
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Ke Liu et al.
Cellular and molecular gastroenterology and hepatology, 13(2), 483-500 (2021-09-26)
Pancreatitis is characterized by acinar cell death and persistent inflammation. Ferroptosis is a type of lipid peroxidation-dependent necrosis, which is negatively regulated by glutathione peroxidase 4. We studied how trypsin, a serine protease secreted by pancreatic acinar cells, affects the
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