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5-Iodowillardiine: Wikis


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IUPAC name
CAS number 140187-25-3
PubChem 447196
Molecular formula C7H8IN3O4
Molar mass 325.06 g mol−1
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
Infobox references

5-Iodowillardiine is a selective agonist for the kainate receptor, with only limited effects at the AMPA receptor.[1] It is selective for kainate receptors composed of GluR5 subunits.[2][3] It is an excitotoxic neurotoxin in vivo,[4][5] but has proved highly useful for characterising the subtypes and function of the various kainate receptors in the brain and spinal cord.[6][7][8]


  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. ^ Swanson GT, Green T, Heinemann SF. Kainate receptors exhibit differential sensitivities to (S)-5-iodowillardiine. Molecular Pharmacology. 1998 May;53(5):942-9. PMID 9584222
  3. ^ Cui C, Mayer ML. Heteromeric kainate receptors formed by the coassembly of GluR5, GluR6, and GluR7. Journal of Neuroscience. 1999 Oct 1;19(19):8281-91. PMID 10493729
  4. ^ Moldrich RX, Cheung NS, Pascoe CJ, Beart PM. Excitotoxic injury profiles of low-affinity kainate receptor agonists in cortical neuronal cultures. European Journal of Pharmacology. 1999 Aug 6;378(2):R1-3. PMID 10478637
  5. ^ Moldrich RX, Beart PM, Pascoe CJ, Cheung NS. Low-affinity kainate receptor agonists induce insult-dependent apoptosis and necrosis in cultured murine cortical neurons. Journal of Neuroscience Research. 2000 Mar 15;59(6):788-96. PMID 10700016
  6. ^ Mascias P, Scheede M, Bloms-Funke P, Chizh B. Modulation of spinal nociception by GluR5 kainate receptor ligands in acute and hyperalgesic states and the role of gabaergic mechanisms. Neuropharmacology. 2002 Sep;43(3):327-39. PMID 12243762
  7. ^ Alt A, Weiss B, Ogden AM, Knauss JL, Oler J, Ho K, Large TH, Bleakman D. Pharmacological characterization of glutamatergic agonists and antagonists at recombinant human homomeric and heteromeric kainate receptors in vitro. Neuropharmacology. 2004 May;46(6):793-806. PMID 15033339
  8. ^ Jane DE, Lodge D, Collingridge GL. Kainate receptors: Pharmacology, function and therapeutic potential. Neuropharmacology. 2008 Aug 28. PMID 18793656


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