期刊
ACS CHEMICAL NEUROSCIENCE
卷 10, 期 3, 页码 1025-1034出版社
AMER CHEMICAL SOC
DOI: 10.1021/acschemneuro.8b00481
关键词
M-5; muscarinic; allosteric modulator; knockout; Alzheimer's disease; schizophrenia; addiction
资金
- NIDA [DA037207]
- William K. Warren Foundation
The muscarinic acetylcholine receptor (mAChR) subtype 5 (M-5) was the most recent mAChR to be cloned and has since emerged as a potential therapeutic target for a number of indications. Early studies with knockout animals have provided clues to the receptor's role in physiological processes related to Alzheimer's disease, schizophrenia, and addiction, and until recently, useful subtype-selective tools to further probe the pharmacology of M-5 have remained elusive. Small-molecule allosteric modulators have since gained traction as a means by which to selectively examine muscarinic pharmacology. This review highlights the discovery and optimization of M-5 positive allosteric modulators (PAMs) and negative allosteric modulators (NAMs).
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