Results 1 to 10 of about 40,413 (202)

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

Pharmaceuticals
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.
Helena Tsimpili, Grigoris Zoidis
doaj   +3 more sources

In Vivo Evaluation of Psoralen in a Copper Sulfate–Induced Chick (Gallus gallus domesticus) Emesis Model and In Silico Analysis of Its Interaction With D2, 5‐HT3A, and Muscarinic Receptors [PDF]

ChemistryOpen
Psoralen (PSN), a naturally occurring furocoumarin, was evaluated for its antiemetic potential using integrated in vivo and in silico approaches, considering the limitations of currently available antiemetic agents.
Kishor Chandra, Sharif Uddin Bahar, Khadija Akter, Mst Muslima Khatun, Samiran Sadhukhan, Progna Saha Puja, Fazley Rohan, Md Shimul Bhuia, Mohammed Alfaifi, Faisal H. Altemani, Faisal Alsenani, Salehin Sheikh, Muhammad Torequl Islam   +12 more
doaj   +3 more sources

M5 positive allosteric modulation alleviates parkinsonian motor deficits. [PDF]

PLoS ONE
Parkinson's disease is a neurodegenerative movement disorder which is characterized by cardinal motor symptoms of tremor at rest, rigidity, bradykineasia, and postural instability.
Nicole E Chambers, Dominic Hall, Morgan Kaplan, Sarah Garan, Tyler Eichner, Mark S Moehle   +5 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

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

Update on the Development of SUVN‐I6107: A True Positive Allosteric Modulator of the Muscarinic M1 Acetylcholine Receptor for the Treatment of Dementia [PDF]

Alzheimers Dement
Background SUVN‐I6107 is a novel and selective muscarinic M1 Positive Allosteric Modulator (PAM) being developed for the treatment of dementia due to neurodegenerative disorders.
Benade V, Shinde A, Badange R, Rasheed M, Subramanian R, Petlu S, Abraham R, Goyal V, Palacharla V, Goura V, Pandey S, Medapati R, Kallepalli R, Nirogi R.   +13 more
europepmc   +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

Synergistic mechanisms of medullary cholinergic-serotonergic pathway interactions in regulating neuronal excitability and locomotor activities [PDF]

Communications Biology
Medullary serotonergic (5-HT) neurons play a pivotal role in locomotor initiation. While these neurons receive cholinergic innervation, the functional consequences and underlying mechanisms remain poorly understood. Using ePet-EYFP transgenic mice (P3–P6)
Yi Cheng, Yue Dai, Renkai Ge, Qiang Zhang   +3 more
doaj   +2 more sources

Synthesis and Evaluation of Fluorinated Peptidomimetics Enabling the Development of ¹⁸F-Labeled Radioligands Targeting Muscarinic Acetylcholine Receptor Subtype M3. [PDF]

ChemMedChem
The muscarinic acetylcholine receptor subtype M3 is validated as a promising target for imaging and therapy in breast cancer. Transcriptomic and proteomic profiling reveal its overexpression, particularly in triple‐negative breast cancer.
Herrera-Rueda MA, Boateng MA, Wuest M, West FG, Wuest F.   +4 more
europepmc   +2 more sources

Muscarinic cannabinoid suppression of excitation, a novel form of coincidence detection [PDF]

Pharmacological Research
Δ9-tetrahydrocannabinol (THC), the chief psychoactive ingredient of cannabis, acts in the brain primarily via cannabinoid CB1 receptors. These receptors are implicated in several forms of synaptic plasticity – depolarization-induced suppression of ...
Michaela Dvorakova, Ken Mackie, Alex Straiker   +2 more
doaj   +2 more sources