SB 242084 monohydrochloride 

SB 242084 monohydrochloride is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C receptor antagonist (crosses the blood-brain barrier). SB 242084 monohydrochloride 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 monohydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage^[1][2][3].

SB 242084 monohydrochloride (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 monohydrochloride (1-100 Nm; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SB 242084 monohydrochloride (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests^[1].
SB 242084 monohydrochloride (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats^[1].
SB 242084 monohydrochloride (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 monohydrochloride (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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

431.32

C₂₁H₂₀Cl₂N₄O₂

1260505-34-7

O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]