1168138-47-3Relevant articles and documents
Discovery of GSK1997132B a novel centrally penetrant benzimidazole PPARγ partial agonist
Sime, Mairi,Allan, Amanda C.,Chapman, Paul,Fieldhouse, Charlotte,Giblin, Gerard M.P.,Healy, Mark P.,Lambert, Millard H.,Leesnitzer, Lisa M.,Lewis, Ann,Merrihew, Raymond V.,Rutter, Richard A.,Sasse, Rosemary,Shearer, Barry G.,Wilson, Timothy M.,Xu, Robert X.,Virley, David J.
, p. 5568 - 5572 (2011/10/09)
The peroxisome proliferator-activated receptor γ (PPARγ) is a ligand-activated nuclear receptor, thought to play a role in energy metabolism, glucose homeostasis and microglia-mediated neuroinflammation. A novel benzimidazole series of centrally penetrant PPARγ partial agonists has been identified. The optimization of PPARγ activity and in vivo pharmacokinetics leading to the identification of GSK1997132B a potent, metabolically stable and centrally penetrant PPARγ partial agonist, is described.
