Abstract:
:Muscarinic acetylcholine receptors mediate diverse physiological functions. At present, five receptor subtypes (M(1) - M(5)) have been identified. The odd-numbered receptors (M(1), M(3), and M(5)) are preferentially coupled to G(q/11) and activate phospholipase C, which initiates the phosphatidylinositol trisphosphate cascade leading to intracellular Ca(2+) mobilization and activation of protein kinase C. On the other hand, the even-numbered receptors (M(2) and M(4)) are coupled to G(i/o), and inhibit adenylyl cyclase activity. They also activate G protein-gated potassium channels, which leads to hyperpolarization of the plasma membrane in different excitable cells. Individual members of the family are expressed in an overlapping fashion in various tissues and cell types. Recent gene targeting approaches have unraveled the specific function of these muscarinic receptor subtypes, which were not able to be fully elucidated with pharmacological approaches because of the non-selective effects of the available ligands. Based on these findings, muscarinic receptors have been emerging as an important therapeutic target for various diseases, including dry mouth, incontinence and chronic obstructive pulmonary disease. Here we review the latest advances in the structural and functional characterization of muscarinic acetylcholine receptors and the pharmaceutical development of muscarinic receptor ligands.
journal_name
Curr Pharm Desjournal_title
Current pharmaceutical designauthors
Ishii M,Kurachi Ydoi
10.2174/138161206778522056subject
Has Abstractpub_date
2006-01-01 00:00:00pages
3573-81issue
28eissn
1381-6128issn
1873-4286journal_volume
12pub_type
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612819666140110122307
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journal_title:Current pharmaceutical design
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,meta分析
doi:10.2174/1381612824666180406104516
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612823666161118144829
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2007-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206775201983
更新日期:2006-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612820666141110164604
更新日期:2015-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210790112674
更新日期:2010-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161212800166031
更新日期:2012-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161210791034021
更新日期:2010-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612826666200212113903
更新日期:2020-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612821666150428125812
更新日期:2015-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/1381612822666160226132630
更新日期:2016-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161206777698945
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
doi:10.2174/138161211795656800
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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pub_type: 杂志文章,评审
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更新日期:2005-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章
doi:10.2174/1381612826999201116163951
更新日期:2020-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2016-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,meta分析,评审
doi:10.2174/1381612822666161010121356
更新日期:2017-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2012-01-01 00:00:00
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journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2006-01-01 00:00:00
abstract::Natural products remain the best resources of drugs and drug leads. Recently, there is growing recognition that identifying new small molecules to promote bone regeneration is a laudable translational goal. In fact, new approaches for bone repair and regeneration that involve inexpensive naturally-derived compounds wo...
journal_title:Current pharmaceutical design
pub_type: 杂志文章,评审
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更新日期:2017-01-01 00:00:00