Positive effects of allosteric modulators on the binding properties and the function of muscarinic acetylcholine receptors |
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| Affiliation: | 1. Institute of Physiology AV CR, Videnská 1083, 14220 Prague, Czech Republic;2. University of Minnesota Medical School, Minneapolis 55455 MN, USA;1. Departments of Pharmacology and Toxicology, Boonshoft School of Medicine at Wright State University, Dayton, OH, 45435, United States;2. Departments of Dermatology, Boonshoft School of Medicine at Wright State University, Dayton, OH, 45435, United States;3. The Dayton V.A. Medical Center, Dayton, OH, 45428, United States;1. Department of Legal Medicine, Kyorin University, School of Medicine, Tokyo, Japan;2. Department of Forensic Medicine and Pathology, Kanazawa University, Graduate School of Medical Sciences, Ishikawa, Japan;3. Department of Neuroanatomy, Kanazawa University, Graduate School of Medical Sciences, Ishikawa, Japan;1. Department of Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University, 46-29 Shimoadachi-cho, Sakyo-ku, Kyoto 606-8501, Japan;2. Department of Pharmacology, Kobe Pharmaceutical University, 4-19-1 Motoyamakita-machi, Higashinada-ku, Kobe 658-8558, Japan;1. Innovation Hub, Cardiff University School of Medicine, University Hospital Wales, Cardiff CF14 4XN, UK;2. Morvus Technology, Aberllech, Pentre Bach, Brecon LD3 8UB, UK |
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| Abstract: | Data are reviewed indicating that allosteric modulators can enhance the affinities of muscarinic receptors for their antagonists and agonists, that the enhancement of the affinity for agonists is relevant functionally, and that the allosterically induced conformational change also affects the interaction between the receptors and the G proteins. |
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