期刊
MOLECULAR BIOSYSTEMS
卷 6, 期 8, 页码 1345-1354出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c002938f
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资金
- NIMH NIH HHS [R01 MH073676] Funding Source: Medline
- NINDS NIH HHS [P50 NS071669] Funding Source: Medline
- NATIONAL INSTITUTE OF MENTAL HEALTH [R01MH073676] Funding Source: NIH RePORTER
- NATIONAL INSTITUTE OF NEUROLOGICAL DISORDERS AND STROKE [P50NS071669] Funding Source: NIH RePORTER
Muscarinic acetylcholine receptors (mAChRs) represent exciting therapeutic targets for the treatment of multiple CNS disorders. The high degree of conservation of amino acids comprising the orthosteric acetylcholine (ACh) binding site between individual mAChR subtypes has hindered the development of subtype-selective compounds that bind to this site. As a result, many academic and industry researchers are now focusing on developing allosteric activators of mAChRs including both positive allosteric modulators (PAMs) and allosteric agonists. In the past 10 years major advances have been achieved in the discovery of allosteric ligands that possess much greater selectivity for individual mAChR subtypes when compared to previously developed orthosteric agents. These novel allosteric modulators of mAChRs may provide therapeutic potential for treatment of a number of CNS disorders such as Alzheimer's disease and schizophrenia.
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