SB 242084 (dihydrochloride)

SB 242084 dihydrochloride is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier) . SB 242084 dihydrochloride increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 dihydrochloride also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 dihydrochloride has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage[1][2][3].

Product Specifications

CAS Number

[1049747-87-6]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Metabolic Disease; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/SB-242084-hydrochloride.html

Concentration

10mM

Purity

98.33

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(N1CCC2=C1C=C(Cl)C(C)=C2)NC3=CC=C(OC4=CC=CN=C4C)N=C3.[H]Cl.[H]Cl

Molecular Formula

C21H21Cl3N4O2

Molecular Weight

467.78

Precautions

H302, H315, H319, H335

References & Citations

[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. |[3]Kennett GA, et al. SB 242084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology. 1997 Apr-May;36 (4-5) :609-20.