A small-molecule antagonist of human and murine CCR1 receptors

Chemokine receptors have been recognised as attractive targets for drug dev elopment. Although the notion that chemokine receptor antagonism can signif icantly reduce inflammation has been supported by evidence obtained with mo dified chemokines and antibodies to chemokines or their receptors, the focu s of most pharmaceutical organisations have been small molecular weight ant agonists. A small molecule antagonist with high affinities to both human an d mouse CCR1 receptors has been prepared by modifications of a lead compoun d, xanthene-9-carboxamide. This molecule also functions as a human CCR3 ant agonist. This molecule should be an important tool in establishing the role of CCR1 and CCR3 receptors in established murine models of disease.