Identification of 2-oxo-N-(phenylmethyl)-4-imidazolidinecarboxamide antagonists of the P2X7 receptor

A backup molecule to compound 2 was sought by targeting the most likely metabolically vulnerable site in this molecule. Compound 18 was subsequently identified as a potent P2X7 antagonist with very low in vivo clearance and high oral bioavailability in all species examined. Some evidence to support the role of P2X7 in the etiology of pain is also presented.

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