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Open Access Articles- Top Results for BAY 73-6691

BAY 73-6691

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BAY 73-6691
File:BAY73-6691 structure.png
Systematic (IUPAC) name
1-(2-chlorophenyl)-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
Clinical data
Identifiers
794568-92-6 7pxY
PubChem CID 16078952
ChemSpider 21171546 7pxY
ChEMBL CHEMBL1513993
Chemical data
Formula C15H12ClF3N4O
356.730 g/mol
 14pxY (what is this?)  (verify)

BAY 73-6691 is a drug developed by Bayer for the treatment of Alzheimer's disease. It was the first compound developed that acts as a phosphodiesterase inhibitor selective for the PDE9A subtype. The PDE9A enzyme is expressed primarily in the brain, with high concentrations in the cerebellum, neocortex, striatum, and hippocampus, and acts to limit the cGMP-mediated signal transduction which occurs following glutamate binding to NMDA receptors. Consequently selective PDE9A inhibitors were predicted to prolong intracellular responses to glutamate and enhance glutamate signalling, and since this process is known to be involved in learning and memory, PDE9A inhibitors should have a nootropic effect and may be useful in the treatment of Alzheimer's.[1]

Animal studies have confirmed these expectations, and BAY 73-6691 has been shown to improve learning and memory in rats.[2] As the first selective PDE9A inhibitor to be developed, it is also widely used in research into the function of this enzyme subtype. However pre-clinical research is at an early stage and it is not yet known whether BAY 73-6691 will prove suitable to progress to human trials, or if it will remain merely a laboratory research tool.


References

  1. ^ Wunder F, Tersteegen A, Rebmann A, Erb C, Fahrig T, Hendrix M. Characterization of the first potent and selective PDE9 inhibitor using a cGMP reporter cell line. Molecular Pharmacology. 2005 Dec;68(6):1775-81. PMID 16150925
  2. ^ van der Staay FJ, Rutten K, Bärfacker L, Devry J, Erb C, Heckroth H, Karthaus D, Tersteegen A, van Kampen M, Blokland A, Prickaerts J, Reymann KG, Schröder UH, Hendrix M. The novel selective PDE9 inhibitor BAY 73-6691 improves learning and memory in rodents. Neuropharmacology. 2008 Oct;55(5):908-18. PMID 18674549