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• W2065351751 abstract "N3-Substitution of the uracil ring of willardiine with a variety of carboxyalkyl or carboxybenzyl substituents produces AMPA and kainate receptor antagonists. In an attempt to improve the potency and selectivity of these AMPA and kainate receptor antagonists a series of analogues with different terminal acidic groups and interacidic group spacers was synthesized and pharmacologically characterized. (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxythiophene-3-ylmethyl)pyrimidine-2,4-dione (43, UBP304) demonstrated high potency and selectivity toward native GLUK5-containing kainate receptors (KD 0.105 ± 0.007 μM vs kainate on native GLUK5; KD 71.4 ± 8.3 μM vs (S)-5-fluorowillardiine on native AMPA receptors). On recombinant human GLUK5, GLUK5/GLUK6, and GLUK5/GLUK2, KB values of 0.12 ± 0.03, 0.12 ± 0.01, and 0.18 ± 0.02 μM, respectively, were obtained for 43. However, 43 displayed no activity on homomeric GLUK6 or GLUK7 kainate receptors or homomeric GLUA1-4 AMPA receptors (IC50 values > 100 μM). Thus, 43 is a potent and selective GLUK5 receptor antagonist." @default.
• W2065351751 created "2016-06-24" @default.
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• W2065351751 date "2006-03-22" @default.
• W2065351751 modified "2023-09-24" @default.
• W2065351751 title "Structure−Activity Relationship Studies on N³-Substituted Willardiine Derivatives Acting as AMPA or Kainate Receptor Antagonists" @default.
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• W2065351751 doi "https://doi.org/10.1021/jm051086f" @default.
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