Synthesis of willardiine and 6-azawillardiine analogs: pharmacological characterization on cloned homomeric human AMPA and kainate receptor subtypes

…, M Deverill, D Bleakman, A Mandelzys

Index: Jane, David E.; Hoo, Ken; Kamboj, Raj; Deverill, Michele; Bleakman, David; Mandelzys, Allan Journal of Medicinal Chemistry, 1997 , vol. 40, # 22 p. 3645 - 3650

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Citation Number: 103

Abstract

Both willardiine and azawillardiine analogs (1 8-28) have been reported to be potent and selective agonists for either AMPA or kainate receptors. We report here the novel synthesis and pharmacological characterization of a range of willardiine (18-23) and 6-azawillardiine (24-28) analogs on cells individually expressing human homomeric hGluR1, hGluR2, hGluR4, or hGluR5 receptors. Reaction of the sodium salts of substituted uracils (7-12) or ...