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Chemical compound
Pharmaceutical compound
SB-228357
Identifiers
  • N-(3-fluoro-5-pyridin-3-ylphenyl)-5-methoxy-6-(trifluoromethyl)-2,3-dihydroindole-1-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC22H17F4N3O2
Molar mass431.391 g·mol−1
3D model (JSmol)
  • COC1=C(C=C2C(=C1)CCN2C(=O)NC3=CC(=CC(=C3)C4=CN=CC=C4)F)C(F)(F)F
  • InChI=1S/C22H17F4N3O2/c1-31-20-9-13-4-6-29(19(13)11-18(20)22(24,25)26)21(30)28-17-8-15(7-16(23)10-17)14-3-2-5-27-12-14/h2-3,5,7-12H,4,6H2,1H3,(H,28,30)
  • Key:RRJLJKRFFRZRAF-UHFFFAOYSA-N

SB-228357 is a drug which acts as a selective antagonist of the serotonin 5-HT2B and 5-HT2C receptors.[1][2]

It has antidepressant and anxiolytic effects in animal models[1][2] and inhibits 5-HT2B mediated proliferation of cardiac fibroblasts.[3] It has also been found to reverse meta-chlorophenylpiperazine (mCPP)-induced hypolocomotion[2] and to attenuate haloperidol-induced catalepsy.[1]

The drug was under development by GlaxoSmithKline for the treatment of major depressive disorder and anxiety disorders. It reached the preclinical research phase of development. However, development of the drug was discontinued.

See also

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References

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  1. 1 2 3 Reavill C, Kettle A, Holland V, Riley G, Blackburn TP (February 1999). "Attenuation of haloperidol-induced catalepsy by a 5-HT2C receptor antagonist". Br J Pharmacol. 126 (3): 572–574. doi:10.1038/sj.bjp.0702350. PMC 1565856. PMID 10188965.
  2. 1 2 3 Bromidge SM, Dabbs S, Davies DT, Davies S, Duckworth DM, Forbes IT, et al. (March 2000). "Biarylcarbamoylindolines are novel and selective 5-HT(2C) receptor inverse agonists: identification of 5-methyl-1-[[2-[(2-methyl-3-pyridyl)oxy]- 5-pyridyl]carbamoyl]-6-trifluoromethylindoline (SB-243213) as a potential antidepressant/anxiolytic agent". Journal of Medicinal Chemistry. 43 (6): 1123–34. doi:10.1021/jm990388c. PMID 10737744.
  3. ↑ Hutcheson JD, Ryzhova LM, Setola V, Merryman WD (November 2012). "5-HT(2B) antagonism arrests non-canonical TGF-β1-induced valvular myofibroblast differentiation". Journal of Molecular and Cellular Cardiology. 53 (5): 707–14. doi:10.1016/j.yjmcc.2012.08.012. PMC 3472096. PMID 22940605.
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