Results 11 to 20 of about 39,843 (183)

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, Patrick R, Gentry, Patricia, Rueda, Sandra, Den Hoedt, Patrick M, Sexton, Christopher J, Langmead, Arthur, Christopoulos   +6 more
semanticscholar   +4 more sources

Crystal structure of the M₅ muscarinic acetylcholine receptor [PDF]

Proceedings of the National Academy of Sciences, 2019
AbstractThe human M5 muscarinic acetylcholine receptor (mAChR) has recently emerged as an exciting therapeutic target for treating a range of disorders, including drug addiction. However, a lack of structural information for this receptor subtype has limited further drug development and validation.
Ziva Vuckovic, Patrick R. Gentry, Alice E. Berizzi, Kunio Hirata, Swapna Varghese, Geoff Thompson, Emma T. van der Westhuizen, Wessel A.C. Burger, Raphaёl Rahmani, Celine Valant, Christopher J. Langmead, Craig W. Lindsley, Jonathan Baell, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos, David M. Thal   +16 more
openaire   +4 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

Regulation of the Muscarinic M3 Receptor by Myocardin-Related Transcription Factors

Frontiers in Physiology, 2021
Myocardin-related transcription factors (MRTFs: myocardin/MYOCD, MRTF-A/MRTFA, and MRTF-B/MRTFB) are co-factors of serum response factor (SRF) that activate the smooth muscle cell (SMC) gene program and that play roles in cardiovascular development and ...
Li Liu, Li Liu, Catarina Rippe, Ola Hansson, Ola Hansson, Dmytro Kryvokhyzha, Steven Fisher, Mari Ekman, Karl Swärd   +8 more
doaj   +2 more sources

M1 muscarinic receptor activation decreases alcohol consumption via a reduction in consummatory behavior

Pharmacology Research & Perspectives, 2022
Muscarinic acetylcholine receptors (mAChRs) have been shown to mediate alcohol consumption and seeking. Both M4 and M5 mAChRs have been highlighted as potential novel treatment targets for alcohol use disorders (AUD).
Leigh C. Walker, Erin J. Campbell, Kate L. Huckstep, Nicola A. Chen, Christopher J. Langmead, Andrew J. Lawrence   +5 more
doaj   +2 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   +1 more source

Activation of Metabotropic Glutamate Receptor (mGlu2) and Muscarinic Receptors (M1, M4, and M5), Alone or in Combination, and Its Impact on the Acquisition and Retention of Learning in the Morris Water Maze, NMDA Expression and cGMP Synthesis

Biomolecules, 2023
The Morris water maze (MWM) is regarded as one of the most popular tests for detecting spatial memory in rodents. Long-term potentiation and cGMP synthesis seem to be among the crucial factors involved in this type of learning. Muscarinic (M1, M4, and M5
J. Wierońska, P. Cieślik, G. Burnat, L. Kalinowski   +3 more
semanticscholar   +1 more source

Chronic Loss of Muscarinic M5 Receptor Function Manifests Disparate Impairments in Exploratory Behavior in Male and Female Mice despite Common Dopamine Regulation

Journal of Neuroscience, 2022
There are five cloned muscarinic acetylcholine receptors (M1–M5). Of these, the muscarinic type 5 receptor (M5) is the only one localized to dopamine neurons in the ventral tegmental area and substantia nigra. Unlike M1–M4, the M5 receptor has relatively
John A. Razidlo, Skylar Fausner, Anna E. Ingebretson, Liuchang Wang, Christopher L. Petersen, Salahudeen Mirza, Isabella N. Swank, V. Alvarez, Julia C. Lemos   +8 more
semanticscholar   +1 more source

A Universal Pharmacological-Based List of Drugs with Anticholinergic Activity

Pharmaceutics, 2023
Anticholinergic burden tools have relevant pharmacological gaps that may explain their limited predictive ability for clinical outcomes. The aim of this study was to provide a universal pharmacological-based list of drugs with their documented affinity ...
Marta Lavrador, Ana C. Cabral, Manuel T. Veríssimo, Fernando Fernandez-Llimos, Isabel V. Figueiredo, M. Margarida Castel-Branco   +5 more
doaj   +1 more source