[CAS NO. 181632-25-7] SB242084
PRODUCTS SPECIFICATIONS [181632-25-7]
DESCRIPTION [181632-25-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 394.85 |
| Molecular Formula | C21H19ClN4O2 |
| SMILES | O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3 |
1 Publications Citing Use of MCE
Summary
SB 242084 is a selective, competitive and high-affinity ( pK i =9.0) 5-HT 2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT 2A receptor . SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage [1] [2] [3] .
IC50 & Target
|
5-HT 2C Receptor 9.0 (pKi) |
In Vitro
SB 242084 (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT
2C
receptor in SH-SY5Y cells
[1]
.
SB 242084 (1-100 Nm; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [1]
| Cell Line: | SH-SY5Y cells |
| Concentration: | 100 nM |
| Incubation Time: | 45 min |
| Result: | Antagonized 5-HT induced concentration-related increase in PI hydrolysis. |
RT-PCR [2]
| Cell Line: | RPTC cells |
| Concentration: | 1-100 nM |
| Incubation Time: | 24 h |
| Result: | Increased FCCP-uncoupled respiration and PGC-1α mRNA expression. |
In Vivo
SB 242084 (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests
[1]
.
SB 242084 (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats
[1]
.
SB 242084 (5, 10 mg/kg; i.p.; single) increases the levels of basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens of rats
[3]
.
SB 242084 (160-640 µg/kg; i.v.; single) dose-dependently and significantly increases the basal firing rate of VTA (ventral tegmental area) dopaminergic neurons, and the bursting activity is also enhanced in the same area, in vivo
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague-Dawley (CD) rats [1] . |
| Dosage: | 0.1-1 mg/kg |
| Administration: | Intraperitoneal injection; single; 20 min pre-test |
| Result: | Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box. |
| Animal Model: | Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model) [1] . |
| Dosage: | 5 mg/kg |
| Administration: | Intraperitoneal injection; single; 20 min pre-test |
| Result: | Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation. |
| Animal Model: | Rats [2] . |
| Dosage: | 5, 10 mg/kg |
| Administration: | Intraperitoneal injection; single |
| Result: | Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 44 mg/mL ( 111.43 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.5326 mL | 12.6630 mL | 25.3261 mL |
| 5 mM | 0.5065 mL | 2.5326 mL | 5.0652 mL |
| 10 mM | 0.2533 mL | 1.2663 mL | 2.5326 mL |
-
1.
-
2.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 2.5 mg/mL (6.33 mM); Clear solution
References
- [1] Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36(4-5):609-20.
- [2] Harmon JL, et al. 5-HT2 Receptor Regulation of Mitochondrial Genes: Unexpected Pharmacological Effects of Agonists and Antagonists. J Pharmacol Exp Ther. 2016 Apr;357(1):1-9.
Synonyms
