P598. Exploring the Molecular Determinants for Functional Selectivity of the Antipsychotic Xanomeline at Muscarinic Acetylcholine Receptors

Biological Psychiatry(2022)

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摘要
Xanomeline (formulated as KarXT) is a selective M1/M4 muscarinic acetylcholine receptor (mAChR) agonist being developed for the treatment of symptoms associated with schizophrenia and Alzheimer’s disease (AD). Questions remain regarding the mechanisms of xanomeline’s selectivity. Therefore, we specifically investigated molecular determinants of xanomeline binding and functional selectivity using two of the most highly homologous Gi-coupled mAChR subtypes (M2/M4).
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关键词
Muscarinic Receptor Agonists, Xanomeline, Preclinical, Mechanism of Action
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