A novel series of antagonists of the human P2X7 receptor is described. Modification of substituents enabled identification of compounds selective for the rat P2X7 receptor and provides useful pharmacological tools for evaluation of the role of P2X7 in disease.
Amidocyclopropanes are readily prepared by reaction of N-diethoxymethyl amides with alkenes in the presence of zinc amagalm, zinc chloride and chlorotrimethylsilane.
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