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5-Fluorowillardiine: Wikis


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IUPAC name
CAS number 140187-23-1
PubChem 126569
Molecular formula C7H8FN3O4
Molar mass 217.15 g mol−1
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
Infobox references

5-Fluorowillardiine is a selective agonist for the AMPA receptor,[1][2][3] with only limited effects at the kainate receptor.[4] It is an excitotoxic neurotoxin when used in vivo and so is rarely used in intact animals, but it is widely used to selectively stimulate AMPA receptors in vitro.[5][6][7]


  1. ^ Patneau DK, Mayer ML, Jane DE, Watkins JC. Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. Journal of Neuroscience. 1992 Feb;12(2):595-606. PMID 1371315
  2. ^ Hawkins LM, Beaver KM, Jane DE, Taylor PM, Sunter DC, Roberts PJ. Characterization of the pharmacology and regional distribution of (S)-[3H]-5-fluorowillardiine binding in rat brain. British Journal of Pharmacology. 1995 Oct;116(3):2033-9. PMID 8640342
  3. ^ Lunn ML, Ganakas AM, Mercer LD, Lawrence AJ, Beart PM. Localisation and properties of AMPA-insensitive kainate sites: receptor autoradiography and gene expression in rat brain. Neuroscience Letters. 1996 Feb 2;204(1-2):121-4. PMID 8929993
  4. ^ Larm JA, Cheung NS, Beart PM. (S)-5-fluorowillardiine-mediated neurotoxicity in cultured murine cortical neurones occurs via AMPA and kainate receptors. European Journal of Pharmacology. 1996 Oct 24;314(1-2):249-54. PMID 8957243
  5. ^ Jensen RJ. Responses of directionally selective retinal ganglion cells to activation of AMPA glutamate receptors. Visual Neuroscience. 1999 Mar-Apr;16(2):205-19. PMID 10367956
  6. ^ Olivera S, Rodriguez-Ithurralde D, Henley JM. Regional localization and developmental profile of acetylcholinesterase-evoked increases in [(3)H]-5-fluororwillardiine binding to AMPA receptors in rat brain. British Journal of Pharmacology. 2001 Aug;133(7):1055-62. PMID 11487516
  7. ^ Kessler M, Arai AC. Use of [3H]fluorowillardiine to study properties of AMPA receptor allosteric modulators. Brain Research. 2006 Mar 3;1076(1):25-41. PMID 16256076


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