A small-molecule antagonist of human and murine CCR1 receptors.

Chemokine receptors have been recognised as attractive targets for drug development. Although the notion that chemokine receptor antagonism can significantly reduce inflammation has been supported by evidence obtained with modified chemokines and antibodies to chemokines or their receptors, the focus of most pharmaceutical organisations have been small molecular weight antagonists. A small molecule antagonist with high affinities to both human and mouse CCR1 receptors has been prepared by modifications of a lead compound, xanthene-9-carboxamide. This molecule also functions as a human CCR3 antagonist. This molecule should be an important tool in establishing the role of CCR1 and CCR3 receptors in established murine models of disease.