Results 191 to 200 of about 19,182 (246)

Cholinergic Mechanisms in Gastrointestinal Neoplasia. [PDF]

Int J Mol Sci
Sampaio Moura N, Schledwitz A, Alizadeh M, Kodan A, Njei LP, Raufman JP.   +5 more
europepmc   +1 more source

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Muscarinic Acetylcholine Receptor M5

Definitions, 2020
Muscarinic acetylcholine receptor M5 (532 aa, ~60 kDa) is encoded by the human CHRM5 gene. This protein plays a role in both acetylcholine binding and G protein-coupled receptor signaling.

semanticscholar   +2 more sources

Identification of a Novel Allosteric Site at the M5 Muscarinic Acetylcholine Receptor

ACS Chemical Neuroscience, 2021
The M5 muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders.
Wessel A. C. Burger, P. Gentry, Alice E. Berizzi, Ziva Vuckovic, E. T. van der Westhuizen, Geoff V. Thompson, M. Yeasmin, C. Lindsley, P. Sexton, C. Langmead, A. Tobin, A. Christopoulos, C. Valant, D. Thal   +13 more
semanticscholar   +3 more sources

The Muscarinic Acetylcholine Receptor M5: Therapeutic Implications and Allosteric Modulation.

ACS Chemical Neuroscience, 2018
The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) was the most recent mAChR to be cloned and has since emerged as a potential therapeutic target for a number of indications.
Aaron M. Bender, Aaron T Garrison, C. Lindsley   +2 more
semanticscholar   +4 more sources

Activation mechanism of the M5 muscarinic acetylcholine receptor.

Biophysical Journal, 2023
Lee Roy, A. D. Vélez, Jokent T. Gaza, Ricky B. Nellas   +3 more
semanticscholar   +2 more sources

An Improved Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor

Synfacts, 2022

semanticscholar   +2 more sources

Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes

Neuron, 1988
The human and rat genes for a fifth muscarinic receptor have been cloned and expressed in mammalian cells. The 532 amino acid human protein has 89% sequence identity to the 531 amino acid rat protein and is most closely related to the m3 receptor. Both proteins are encoded by single exons.
T. Bonner, A. Young, Mark R. Bran, N. Buckley   +3 more
semanticscholar   +4 more sources

Development of VU6019650: A Potent, Highly Selective, and Systemically Active Orthosteric Antagonist of the M5 Muscarinic Acetylcholine Receptor for the Treatment of Opioid Use Disorder.

Journal of Medicinal Chemistry, 2022
The muscarinic acetylcholine receptor (mAChR) subtype 5 (M5) represents a novel potential target for the treatment of multiple addictive disorders, including opioid use disorder.
Aaron T Garrison, Douglas L. Orsi, Rory A. Capstick, David Whomble, Jinming Li, Trever R. Carter, Andrew S. Felts, P. Vinson, Alice L. Rodriguez, Allie Han, Krishma Hajari, Hyekyung P. Cho, Laura B. Teal, Madeline G Ragland, M. Ghamari-Langroudi, M. Bubser, Sichen Chang, N. Schnetz-Boutaud, O. Boutaud, Anna L Blobaum, Daniel J. Foster, C. Niswender, P. Conn, C. Lindsley, Carrie K Jones, Changho Han   +25 more
semanticscholar   +1 more source

Discovery of M5 Muscarinic Acetylcholine Receptor Antagonists: 1‐Methyl‐4‐Phenylpiperidine Analogs

The FASEB Journal, 2015
Na-Ra Lee, Xuan Zhang, M. Darna, Guangrong Zheng, L. Dwoskin   +4 more
semanticscholar   +2 more sources

Characterization of methanthelinium binding and function at human M1–M5 muscarinic acetylcholine receptors [PDF]

Naunyn-Schmiedeberg's Archives of Pharmacology, 2018
Firstly, it was determined whether methanthelinium bromide (MB) binds to human M1-M5 (hM1-hM5) muscarinic acetylcholine receptors in comparison to the classical muscarinic antagonist N-methylscopolamine (NMS). [3H]NMS dissociation binding experiments revealed an allosteric retardation of dissociation at 100 μM of MB ranging from none in hM3 to 4.6-fold
Matthias Irmen, Janine Holze, Theresa Bödefeld, Christian Tränkle   +3 more
openaire   +2 more sources