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Front Cover: Synthesis and Preliminary Evaluation of 11 C‐Labeled VU0467485/AZ13713945 and Its Analogues for Imaging Muscarinic Acetylcholine Receptor Subtype 4 (ChemMedChem 3/2019)
Author(s) -
Deng Xiaoyun,
Hatori Akiko,
Chen Zhen,
Kumata Katsushi,
Shao Tuo,
Zhang Xiaofei,
Yamasaki Tomoteru,
Hu Kuan,
Yu Qingzhen,
Ma Longle,
Wang Gangqiang,
Wang Lu,
Shao Yihan,
Josephson Lee,
Sun Shaofa,
Zhang MingRong,
Liang Steven
Publication year - 2019
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201900047
Subject(s) - muscarinic acetylcholine receptor , allosteric modulator , acetylcholine , agonist , allosteric regulation , chemistry , neuroscience , acetylcholine receptor , front cover , neurotransmitter , receptor , biophysics , pharmacology , cover (algebra) , biochemistry , psychology , medicine , biology , mechanical engineering , engineering
The Front Cover shows three 11 C‐labeled positron emission tomography (PET) ligands based on a validated M 4 R positive allosteric modulator VU0467485 (AZ13713945). Five distinct subunits (M 1 –M 5 ) of muscarinic acetylcholine receptors (mAChRs) are involved in the action of the neurotransmitter acetylcholine in the central and peripheral nervous system. Attributed to promising clinical efficacy of an M 1 /M 4 ‐preferring agonist Xanomeline in schizophrenic and Alzheimer's patients, M 1 or M 4 ‐selective mAChR modulators have been developed that target the topographically distinct allosteric sites. Therefore, we developed prototype PET ligands to visualize the M 4 target in the brain and provide preliminary evaluation of these novel chemical scaffolds for further medicinal chemistry development. More information can be found in the Communication by Shaofa Sun, Ming‐Rong Zhang, Steven Liang et al. on page 303 in Issue 3, 2019 (DOI: 10.1002/cmdc.201800710).