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SB 242084 dihydrochloride 

Cat. No. M27717
SB 242084 dihydrochloride  Structure
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Biological Activity

SB 242084 dihydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage.

Chemical Information
Molecular Weight 467.78
Formula C21H21Cl3N4O2
CAS Number 1049747-87-6
Form Solid
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Parthena Martin, et al. Epilepsy Behav. Fenfluramine modulates the anti-amnesic effects induced by sigma-1 receptor agonists and neuro(active)steroids in vivo

[2] Daniel F Manvich, et al. J Pharmacol Exp Ther. The serotonin 2C receptor antagonist SB 242084 exhibits abuse-related effects typical of stimulants in squirrel monkeys

[3] Avi E Zayara, et al. Psychopharmacology (Berl). Blockade of nucleus accumbens 5-HT2A and 5-HT2C receptors prevents the expression of cocaine-induced behavioral and neurochemical sensitization in rats

[4] Elizabeth A Hackler, et al. J Pharmacol Exp Ther. 5-Hydroxytryptamine2C receptor contribution to m-chlorophenylpiperazine and N-methyl-beta-carboline-3-carboxamide-induced anxiety-like behavior and limbic brain activation

[5] Mihaly Hajos, et al. J Pharmacol Exp Ther. Regulation of septo-hippocampal activity by 5-hydroxytryptamine(2C) receptors

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