Discovery and Development of Muscarinic Acetylcholine M₄ Activators as Promising Therapeutic Agents for CNS Diseases
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- Takai Kentaro
- Drug Research Division, Sumitomo Dainippon Pharma Co., Ltd.
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- Enomoto Takeshi
- Drug Research Division, Sumitomo Dainippon Pharma Co., Ltd.
書誌事項
- タイトル別名
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- Discovery and Development of Muscarinic Acetylcholine M<sub>4</sub> Activators as Promising Therapeutic Agents for CNS Diseases
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<p>Among the muscarinic acetylcholine receptor (mAChR) subtypes, the M4 receptor has been investigated as a promising drug target for the treatment of schizophrenia. These investigations have been based on findings from M4-deficient mice studies as well as on the results of a clinical trial that used xanomeline, an M1/M4 mAChRs-preferring agonist. Both orthosteric agonists and positive allosteric modulators of M4 mAChR have been reported as promising ligands that not only have antipsychotic effects, but can also improve cognitive impairment and motor dysfunction. However, challenges remain due to the high homology of the orthosteric binding site among all muscarinic receptors. In this review, we summarize our approach to the identification of M4 mAChR activators, orthosteric agonists, and positive allosteric modulators based on M4 mAChR structural information and structure–activity relationship studies. These findings indicate that selective M4 mAChR activators are promising potential therapeutic agents for several central nervous system conditions.</p>
収録刊行物
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- CHEMICAL & PHARMACEUTICAL BULLETIN
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CHEMICAL & PHARMACEUTICAL BULLETIN 66 (1), 37-44, 2018
公益社団法人 日本薬学会
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詳細情報 詳細情報について
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- CRID
- 1390282679154644096
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- NII論文ID
- 130006301009
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- NII書誌ID
- AA00602100
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- ISSN
- 13475223
- 00092363
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- NDL書誌ID
- 028738746
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- PubMed
- 29311510
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 使用不可