ChemicalBook > CAS DataBase List > SB 242084 (hydrochloride)

SB 242084 (hydrochloride)

CAS No.1049747-87-6
Chemical Name:SB 242084 (hydrochloride)
CBNumber:CB82592406
Molecular Formula:C21H21Cl3N4O2
Formula Weight:467.77604
MOL File:1049747-87-6.mol

SB 242084 (hydrochloride) Property

storage temp. Sealed in dry,Room Temperature
solubility Ethanol:1.0(Max Conc. mg/mL);2.14(Max Conc. mM)
PBS (pH 7.2):10.0(Max Conc. mg/mL);21.38(Max Conc. mM)
DMSO:59.63(Max Conc. mg/mL);127.47(Max Conc. mM)
DMF:30.0(Max Conc. mg/mL);64.13(Max Conc. mM)
form A crystalline solid
color Off-white to light yellow

Safety

NFPA 704:

	0
2		0

Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal wordWarning
Hazard statements H315-H319-H335
Precautionary statements P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501

SB 242084 (hydrochloride) Chemical Properties,Usage,Production

Description Serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter that activates specific receptors located primarily in the gut and central nervous system. SB-242084 is an antagonist of the 5-HT_2C receptor (pK_i = 9.0), with at least 100-fold more selectivity over other 5-HT, dopamine, or adrenergic receptors. In vivo, it is brain penetrant and has significant anxiolytic activity, without sedative, proconvulsant, or hyperphagic properties. SB-242084 has been used extensively in animal research to evaluate, for example, 5-HT_2C receptor agonists and neurotransmitter receptor interactions in mice.
Uses SB 242084 Hydrochloride is an antagonist of the SR-2C.
Definition ChEBI: 6-chloro-5-methyl-N-[6-(2-methylpyridin-3-yl)oxypyridin-3-yl]-2,3-dihydroindole-1-carboxamide;dihydrochloride is an organic molecular entity, an indole alkaloid and a pyridine. It has a role as a receptor modulator.

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].

Animal Model:	Male Sprague-Dawley (CD) rats^[1].
Dosage:	0.1-1 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliartest box.

Animal Model:	Male Sprague-Dawley (CD) rats(mCPP-induced hypophagia model)^[1].
Dosage:	5 mg/kg
Administration:	Intraperitoneal injection; single; 20 min pre-test
Result:	Significantly reduced the amount of food consumed by 23 h food-deprivedrats over a 1hr test period from the time of food presentation.

Animal Model:	Rats^[2].
Dosage:	5, 10 mg/kg
Administration:	Intraperitoneal injection; single
Result:	Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.

IC 50 5-HT_2C Receptor: 9.0 (pKi)
storage Desiccate at +4°C