Results 1 to 10 of about 19,976 (189)

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   +4 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   +4 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   +4 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

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).
Laura B. Teal, M. Bubser, Edith Duncan, Robert W. Gould, C. Lindsley, Carrie K Jones   +5 more
semanticscholar   +3 more sources

Muscarinic acetylcholine receptor M5 is 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.
Xiao Han, Cong Zhang, Xiangping Ma, Xiaowei Yan, Bohui Xiong, W. Shen, S. Yin, Hongfu Zhang, Qingyuan Sun, Yong Zhao   +9 more
semanticscholar   +3 more sources

Long-Term—But Not Short-Term—Plasticity at the Mossy Fiber–CA3 Pyramidal Cell Synapse in Hippocampus Is Altered in M1/M3 Muscarinic Acetylcholine Receptor Double Knockout Mice

Cells, 2023
Muscarinic acetylcholine receptors are well-known for their crucial involvement in hippocampus-dependent learning and memory, but the exact roles of the various receptor subtypes (M1–M5) are still not fully understood.
Fang Zheng, Jürgen Wess, Christian Alzheimer   +2 more
doaj   +2 more sources

Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias

Frontiers in Pharmacology, 2021
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen, K. H. Christopher Choy, Celine Valant, Simon McKenzie-Nickson, Sophie J. Bradley, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos   +7 more
doaj   +2 more sources

A New Era of Muscarinic Acetylcholine Receptor Modulators in Neurological Diseases, Cancer and Drug Abuse. [PDF]

Pharmaceuticals (Basel)
The cholinergic pathways in the central nervous system (CNS) play a pivotal role in different cognitive functions of the brain, such as memory and learning.
Tsimpili H, Zoidis G.
europepmc   +2 more sources

Characterization of Selective M5 Acetylcholine Muscarinic Receptor Modulators on Dopamine Signaling in the Striatum

The Journal of Pharmacology and Experimental Therapeutics, 2023
The type-5 muscarinic acetylcholine receptor (mAChR, M5) is almost exclusively expressed in dopamine (DA) neurons of the ventral tegmental area and substantia nigra pars compacta; therefore, they are ideally located to modulate DA signaling and ...
Vivien Zell, G. Teuns, A. S. Needham, Sruti Mukherjee, Nathaniel Roscoe, Michelle Le, L. Fourgeaud, G. Woodruff, Anindya Bhattacharya, M. Marella, Pascal Bonaventure, Wayne C. Drevets, B. Balana   +12 more
semanticscholar   +3 more sources