SB 242084

SKU: orb1225878

Description

SB 242084 is a potent, selective, brain penetrant 5-HT2C receptor antagonist with pKi of 9.0, 100- and 158-fold selectivity over the closely related 5-HT2B and 5-HT2A subtypes; also displays >100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors; inhibits 5-HT-stimulated phosphatidylinositol hydrolysis with pKb of 9.3 in cell-baed assays; potently inhibits m-chlorophenylpiperazine (mCPP)-induced hypolocomotion in rats, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o.

Key Properties

• CAS Number: 181632-25-7
• MW: 467.78
• Purity: >98% (HPLC)
• Formula: C₂₁H₁₉ClN₄O₂
• SMILES: CC1=CC2=C(C=C1Cl)N(CC2)C(=O)NC3=CN=C(C=C3)OC4=C(N=CC=C4)C.Cl.Cl
• Target: 5-HT Receptor
• Solubility: DMSO: ≥ 44 mg/mL

Bioactivity

• In Vivo:
  Animal model: Male Sprague-Dawley (CD) rats. 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). 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. Dosage: 5, 10 mg/kg. Administration: Intraperitoneal injection; single. Result: Significantly increased basal dialysate dopamine (DA) and dihydroxyphenylacetic acid (DOPAC) in the nucleus accumbens.
• In Vitro:
  Cell Viability Assay Cell line: SH-SY5Y cells. Concentration: 100 nM. Incubation time: 45 min. Result: Antagonized 5-HT induced concentration-related increase in PI hydrolysis. RT-PCR Cell line: RPTC cells. Concentration: 1-100 nM. Incubation time: 24 h. Result: Increased FCCP-uncoupled respiration and PGC-1α mRNA expression.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SB-242084 | SB242084

Quick Database Links

Gene Symbol

5-HT Receptor