SB 242084 monohydrochloride
Based on 6 publication(s) in Google Scholar
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.
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- CAS No.: 1260505-34-7
- Formula: C21H20Cl2N4O2
- Molecular Weight:431.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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- References
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Publications Citing Use of MedChemExpress (MCE) SB 242084 monohydrochloride
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Biological Activity
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5-HT2A Receptor |
5-HT2C Receptor |
SB 242084 monohydrochloride (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 monohydrochloride (1-100 Nm; 24 h) increases RPTC respiration and PGC-1α mRNA expression in RPTC[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1260505-34-7
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Molecular Weight 431.32
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Formula C21H20Cl2N4O2
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SMILES
O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3.[H]Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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Brain
Hippocampal excitation-inhibition balance underlies the 5-HT2C receptor in modulating depressive behaviours. [Abstract]2024 Nov 4;147(11):3764-3779. PMID: 38701344 -
Biochem Pharmacol
Complement C3/C3a-CCL9 feedback loop orchestrates inflammatory crosstalk to accelerate aortic dissection. [Abstract]2025 Oct 13:117421. PMID: 41093012 -
Eur J Pharmacol
2,5-Dimethoxy-4-methylamphetamine (DOM)-induced gait alterations in mice: Dissecting the role of 5-HT2A/2C receptor-mediated mechanisms. [Abstract]2025 Nov 5:1006:178170. PMID: 40962017 -
Biochem Biophys Res Commun
AMPA receptor potentiation alleviates NLRP3 knockout-induced fear generalization in mice. [Abstract]2024 Aug 30:722:150074. PMID: 38805785 -
Neuroendocrinology
Peripheral 5-HT mediates GnIH-induced feeding behavior and energy metabolism disorder in chickens via the 5-HT2C receptor. [Abstract]2024;114(8):749-774. PMID: 38718758 -
Purity & Documentation
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SB 242084 monohydrochloride Related Classifications
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