(S)-Willardiine
AMPA / kainate receptor agonist （AMPA/红藻氨酸受体拮抗剂）
Purity: >98%
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
Patneau et al (1992) Activation and desensitization of AMPA/kainate receptors by novel derivatives of willardiine. J.Neurosci. 12:595-606 abstract
Hawkins et al (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
Stensbol et al (2002) The AMPA receptor binding site: focus on agonists and competitive antagonists. Curr.Pharm.Design 8:857-872 abstract
Jane et al (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
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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
Chemical Information
(S)-2-Amino-3-(3,4-dihydro-2,4-dioxopyrimidin-1(2H)-yl)propanoic acid
