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(<em>S</em>)-5-Fluorowillardiine

Potent, selective AMPA agonist

Product Code: Asc-036

Purity: >99%

 
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Biological Description

Potent, selective AMPA receptor agonist. Displays higher affinity than AMPA at hGluR1 and hGlurR2, and displays greater selectivity for AMPA receptor subtypes over the kainate receptor hGluR5.

Useful References

(1997) Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes. J.Med.Chem. 40: 3645 abstract

(1995) Binding of the new radioligand (S)-[3H]-AMPA to rat brain synaptic membranes: effects of a series of structural analogues of the non-NMDA receptor agonist willardiine. Neuropharmacol. 34:405 abstract

(1994) Willardiines differentiate agonist binding sites for kainate- versus AMPA-preferring glutamate receptors in DRG and hippocampal neurons. J.Neurosci. 14: 3881 abstract

Citations

Mankiewicz et al (2008) Chemical interplay in the mechanism of partial agonist activation in alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptors. Biochemistry. 47:398-404. abstract

Structure of the S1S2 glutamate binding domain of GluR3 abstract

Probing the allosteric modulator binding site of GluR2 with thiazide derivatives abstract

Chemical Information

(S)-2-Amino-3-(5-fluoro-3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)propanoic acid

Asc-036
  • Desiccate at +4°C
  • MW 217.16
  • Soluble in 1.1 eq. NaOH to 50 mM (with warming)
  • C7H8FN3O4
  • 140187-23-1