期刊
ACS CHEMICAL NEUROSCIENCE
卷 8, 期 3, 页码 435-443出版社
AMER CHEMICAL SOC
DOI: 10.1021/acschemneuro.7b00001
关键词
Xanomeline; muscarinic acetylcholine receptors; Alzheimer's disease; schizophrenia; allosteric modulation; antipsychotic
资金
- NIH
- NIMH [MH082867, MH106839]
Xanomeline (1) is an orthosteric muscarinic acetylcholine receptor (mAChR) agonist, often referred to as M-1/M-4-preferring, that received widespread attention for its clinical efficacy in schizophrenia and Alzheimer's disease (AD) patients. Despite the compound's promising initial clinical results, dose-limiting side effects limited further clinical development. While xanomeline, and related orthosteric muscarinic agonists, have yet to receive approval from the FDA for the treatment of these CNS disorders, interest in the compound's unique M1/M4-preferring mechanism of action is ongoing in the field of chemical neuroscience. Specifically, the promising cognitive and behavioral effects of xanomeline in both schizophrenia and AD have spurred a renewed interest in the development of safer muscarinic ligands with improved subtype selectivity for either M-1 or M-4. This Review will address xanomeline's overall importance in the field of neuroscience, with a specific focus on its chemical structure and synthesis, pharmacology, drug metabolism and pharmacokinetics (DMPK), and adverse effects.
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