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(<em>S</em>)-Willardiine

AMPA / kainate receptor agonist

Product Code: Asc-040

Purity: >98%

 
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Biological Description

Selective AMPA receptor agonist at hGluR1 (Ki = 0.39 μM). Selective over hGluR2 (Ki = 0.90 μM), hGluR4 (Ki = 8.85 μM) and kainate receptor hGluR5 (Ki = 28.9 μM). Produces strong desensitisation.

Useful References

(1992) Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J.Neurosci. 12:595-606 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. 34:405-410 abstract

(2002) The AMPA receptor binding site: focus on agonists and competitive antagonists. Curr.Pharm.Design 8:857-872 abstract

(1997) Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes. J Med Chem 40: 3645-50 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

Chemical Information

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

Asc-040
  • Desiccate at +4°C
  • MW 199.17
  • Soluble in 1.1 eq. NaOH to 50 mM
  • C7H9N3O4
  • 21416-43-3