Results 1 to 10 of about 13,887 (182)

Molecular Conversion of Muscarinic Acetylcholine Receptor M5 to Muscarinic Toxin 7 (MT7)-Binding Protein [PDF]

Toxins, 2011
Muscarinic toxin 7 (MT7) is a mamba venom peptide that binds selectively to the M1 muscarinic acetylcholine receptor. We have previously shown that the second (ECL2) and third (ECL3) extracellular loops of the M1 receptor are critically involved in ...
Katja Näreoja, Johnny Näsman, Sergio Rondinelli   +2 more
doaj   +7 more sources

Muscarinic acetylcholine receptor M5 is involved in spermatogenesis through the modification of cell-cell junctions. [PDF]

Reproduction, 2021
Muscarinic acetylcholine receptor (mAChR) antagonists have been reported to decrease male fertility; however, the roles of mAChRs in spermatogenesis and the underlying mechanisms are not understood yet. During spermatogenesis, extensive remodeling between Sertoli cells and/or germ cells interfaces takes place to accommodate the transport of developing ...
Han X, Zhang C, Ma X, Yan X, Xiong B, Shen W, Yin S, Zhang H, Sun Q, Zhao Y.   +9 more
europepmc   +5 more sources

Muscarinic Acetylcholine Receptor M5 Involved in Spermatogenesis through the Modification of Cell-Cell Junctions [PDF]

Reproduction, 2020
Muscarinic acetylcholine receptor (mAChR) antagonists have been reported to decrease male fertility; however, the roles of mAChRs in spermatogenesis and the underlying mechanisms are not understood yet.
Yong Zhao, Xiao Han, Pengfei Zhang, Wei Shen, Hongfu Zhang, Cong Zhang, Bohui Xiong, Shen Yin, Zhao‐Jia Ge   +8 more
semanticscholar   +5 more sources

Selective M5 muscarinic acetylcholine receptor negative allosteric modulator VU6008667 blocks acquisition of opioid self-administration

Neuropharmacology, 2023
Recent evidence suggests that inhibition of the M5 muscarinic acetylcholine receptor (mAChR) may provide a novel non-opioid mechanism for the treatment of opioid use disorder (OUD). Previous studies from our group and others have demonstrated that acute administration of the long-acting M5 negative allosteric modulator (NAM) ML375 attenuates ...
Laura B. Teal, Michael Bubser, Edith Duncan, Robert W. Gould, Craig W. Lindsley, Carrie K. Jones   +5 more
semanticscholar   +4 more sources

Microscopic Binding of M5 Muscarinic Acetylcholine Receptor with Antagonists by Homology Modeling, Molecular Docking, and Molecular Dynamics Simulation [PDF]

The Journal of Physical Chemistry B, 2011
By performing homology modeling, molecular docking, and molecular dynamics (MD) simulations, we have developed three-dimensional (3D) structural models of the M5 muscarinic acetylcholine receptor (mAChR) and two complexes for M5 mAChR binding with ...
Xiaoqin Huang, Guangrong Zheng, Chang‐Guo Zhan   +2 more
semanticscholar   +5 more sources

Discovery of the First Highly M5-Preferring Muscarinic Acetylcholine Receptor Ligand, an M5 Positive Allosteric Modulator Derived from a Series of 5-Trifluoromethoxy N-Benzyl Isatins [PDF]

Journal of Medicinal Chemistry, 2009
This report describes the discovery and initial characterization of the first positive allosteric modulator of muscarinic acetylcholine receptor subtype 5 (mAChR5 or M5).
Thomas M. Bridges, Joy E. Marlo, Colleen M. Niswender, Carrie K. Jones, Satyawan Jadhav, Patrick R. Gentry, Hyekyung C. Plumley, C. David Weaver, P. Jeffrey Conn, Craig W. Lindsley   +9 more
semanticscholar   +5 more sources

Activation mechanism of the M5 muscarinic acetylcholine receptor

Biophysical Journal, 2023
Lee Roy, A. De Velez, Jokent T. Gaza, Ricky B. Nellas   +3 more
semanticscholar   +3 more sources

Loss of M5 muscarinic acetylcholine receptors leads to cerebrovascular and neuronal abnormalities and cognitive deficits in mice

Neurobiology of Disease, 2006
The M5 muscarinic acetylcholine receptor (M5R) has been shown to play a crucial role in mediating acetylcholine-dependent dilation of cerebral blood vessels.
Runa Araya, Takanori Noguchi, Munehiro Yuhki, Naohito Kitamura, Makoto Higuchi, Takaomi C. Saido, Kenjiro Seki, Shigeyoshi Itohara, Masako Kawano, Kentaro Tanemura, Akihiko Takashima, Kazuyuki Yamada, Yasushi Kondoh, Iwao Kanno, Jürgen Wess, Masahisa Yamada   +15 more
doaj   +5 more sources

Crystal structure of the M5 muscarinic acetylcholine receptor [PDF]

Proceedings of the National Academy of Sciences, 2019
Significance The 5 subtypes of the muscarinic acetylcholine receptors (mAChRs) are expressed throughout the central and peripheral nervous system where they play a vital role in physiology and pathologies. Recently, the M5 mAChR subtype has emerged as an
Ziva Vuckovic, P. Gentry, Alice E. Berizzi, K. Hirata, Swapna Varghese, Geoff V. Thompson, E. T. van der Westhuizen, Wessel A. C. Burger, Raphaël Rahmani, C. Valant, C. Langmead, C. Lindsley, J. Baell, A. Tobin, P. Sexton, A. Christopoulos, D. Thal   +16 more
semanticscholar   +7 more sources

Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators [PDF]

Molecular Pharmacology, 2016
Recently, the first subtype-selective allosteric modulators of the M5 muscarinic acetylcholine receptor (mAChR) have been described, but their molecular mechanisms of action remain unknown. Using radioligand-binding and functional assays of inositol phosphate (IP) accumulation and Ca(2+) mobilization in a recombinant cell line stably expressing the ...
Alice E. Berizzi, P. Gentry, P. Rueda, Sandra Den Hoedt, P. Sexton, C. Langmead, A. Christopoulos   +6 more
semanticscholar   +3 more sources