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Utilizing a combination of high-throughput and multi-step synthesis, SAR in a novel series of M 1 acetylcholine receptor antagonists was rapidly established. The efforts led to the discovery the highly potent M 1 antagonists 6 (VU0431263), and 8f (VU0433670). Functional Schild analysis and radioligand displacement experiments demonstrated the competitive, orthosteric binding of these...
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