SB 242084 (dihydrochloride)

SB 242084 dihydrochloride is a selective, competitive and high-affinity (pK_i=9.0) 5-HT_2C 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-HT_2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage^[1][2][3]. In Vitro:SB 242084 dihydrochloride (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 dihydrochloride (1-100 nM; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC^[2]. In Vivo:SB 242084 dihydrochloride (0.1-1 mg/kg; i.p.; single; 20 min pre-test) improves the behavior of rats in social interaction tests^[1].
SB 242084 dihydrochloride (5 mg/kg; i.p.; single; 20 min pre-test) improves mCPP-induced hypophagia in rats^[1].
SB 242084 dihydrochloride (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 dihydrochloride (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].