Key result
Novel adamantane-based P2X7 receptor antagonists were identified as potent and selective inhibitors of human and rat receptors, providing pharmacological tools to evaluate P2X7 in disease.
The study identifies novel adamantane-based small-molecule P2X7 receptor antagonists that are selective for the rat P2X7 receptor, providing tools for future disease modeling.
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These antagonists supply selective tools for P2X7 research in rat models; leaves open translation to human cardiovascular disease.
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.
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Furber et al. (2007) studied this question. Novel adamantane-based P2X7 receptor antagonists were identified as potent and selective inhibitors of human and rat receptors, providing pharmacological tools to evaluate P2X7 in disease.
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