| Identification | Back Directory | [Name]
SB 242084 hydrochloride | [CAS]
1260505-34-7 | [Synonyms]
SB 242084 hydrochloride,
6-Chloro-5-methyl-N-{6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl}-1-indolinecarboxamide hydrochloride | [Molecular Formula]
C21H20Cl2N4O2 | [MDL Number]
MFCD07363965 | [MOL File]
1260505-34-7.mol | [Molecular Weight]
431.32 |
| Hazard Information | Back Directory | [Uses]
SB 242084 monohydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C 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-HT2A 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]. | [Biological Activity]
Primary Target
5-HT2C | [in vivo]
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]. | [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. DOI:10.1016/s0028-3908(97)00038-5
[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. DOI:10.1124/jpet.115.228395 |
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