SB 242084 (hydrochloride)

Product NameSB 242084 (hydrochloride)
CAS1049747-87-6
MFC21H21Cl3N4O2
MW467.77604
EINECS
MOL File1049747-87-6.mol

Chemical Properties

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

Usage And Synthesis

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

References

[1] G.A. KENNETT . SB 242084, a Selective and Brain Penetrant 5-HT2C Receptor Antagonist[J]. Neuropharmacology, 1997, 36 4: Pages 609-620. DOI: 10.1016/s0028-3908(97)00038-5
[2] STEVEN M. BROMIDGE. 6-Chloro-5-methyl-1-[[2-[(2-methyl-3- pyridyl)oxy]-5-pyridyl]carbamoyl]indoline (SB-242084): The First Selective and Brain Penetrant 5-HT2C Receptor Antagonist[J]. Journal of Medicinal Chemistry, 1997, 40 22: 3494-3496. DOI: 10.1021/jm970424c
[3] PAUL J FLETCHER Guy A H Judy Sinyard. The effects of the 5-HT(2C) receptor antagonist SB242084 on locomotor activity induced by selective, or mixed, indirect serotonergic and dopaminergic agonists.[J]. Psychopharmacology, 2006, 187 4: 515-525. DOI: 10.1007/s00213-006-0453-9
[4] G L DALTON. Serotonin 1B and 2C receptor interactions in the modulation of feeding behaviour in the mouse.[J]. Psychopharmacology, 2006, 185 1: 45-57. DOI: 10.1007/s00213-005-0212-3
[5] JIANPING CHEN, JIA ZHOU* Discovery of Novel Oleamide Analogues as Brain-Penetrant Positive Allosteric Serotonin 5-HT2C Receptor and Dual 5-HT2C/5-HT2A Receptor Modulators[J]. Journal of Medicinal Chemistry, 2023, 66 14: 9992-10009. DOI: 10.1021/acs.jmedchem.3c00908

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