SB 242084_product_DataBase

Bioactivity

SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C 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-HT2A 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].

Invitro

SB 242084 (100 nM; 45 min) exhibits antagonism of the 5-HT stimulated increase in phosphatidylinositol hydrolysis at the human 5-HT2C receptor in SH-SY5Y cells[1].SB 242084 (1-100 Nm; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC[2]. Cell Viability Assay[1] Cell Line:

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]. Animal Model:

Name

SB 242084

CAS

181632-25-7

Formula

C21H19ClN4O2

Molar Mass

394.85

Appearance

Solid

Transport

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

Reference

[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.

PeptideDB

SB 242084

CAS: 181632-25-7 F: C21H19ClN4O2 W: 394.85