Girish Mahajan (Editor)

SB 271046

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PubChem CID
  
5312149

ChemSpider
  
4471579

Formula
  
C20H22ClN3O3S2

Molar mass
  
451.989 g/mol

IUPHAR/BPS
  
276

ChEMBL
  
CHEMBL431298

3D model (Jmol)
  
Interactive image

SB-271046 httpsuploadwikimediaorgwikipediacommonsthu

SB-271046 is a drug which is used in scientific research. It was one of the first selective 5-HT6 receptor antagonists to be discovered, and was found through high-throughput screening of the SmithKline Beecham Compound Bank using cloned 5-HT6 receptors as a target, with an initial lead compound being developed into SB-271046 through a structure-activity relationship (SAR) study. SB-271046 was found to be potent and selective in vitro and had good oral bioavailability in vivo, but had poor penetration across the blood–brain barrier, so further SAR work was then conducted, which led to improved 5-HT6 antagonists such as SB-357,134 and SB-399,885.

SB-271046 was found to increase levels of the excitatory amino acid neurotransmitters glutamate and aspartate, as well as dopamine and noradrenaline in the frontal cortex and hippocampus of rats, and 5-HT6 antagonists have been shown to produce nootropic effects in a variety of animal studies. Suggested applications of these drugs include treatment of schizophrenia and other psychiatric disorders.

References

SB-271046 Wikipedia


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