Results 1 to 10 of about 19,182 (246)

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   +5 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

Downstream Signaling of Muscarinic M₄ Receptors Is Regulated by Receptor Density and Cellular Environment. [PDF]

Pharmacol Res Perspect
ABSTRACT Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators. Considering the importance of comprehending M4 receptor pharmacology for these therapeutic applications, this study investigates M4 receptor ...
Merz M, Playle C, Palchaudhuri M, Hucke O, Gross U, Ursu D.   +5 more
europepmc   +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

Design, Synthesis, and Evaluation of a New Fluorescent Ligand for the M₂ Muscarinic Acetylcholine Receptor. [PDF]

ACS Med Chem Lett
The M2 muscarinic acetylcholine receptor (M2R) is a G protein-coupled receptor involved in regulating cardiovascular functions and mediation of central muscarinic effects, such as movement, temperature control, and antinociceptive responses.
Szabó R, Szepesi Kovács D, Kiss DJ, Yazdi ZN, Tóth AD, Brea J, Loza MI, Meszéna D, Wittner L, Ulbert I, Volk B, Hunyady L, Keserű GM.   +12 more
europepmc   +2 more sources

Light-Activated Pharmacological Tools for Exploring the Cholinergic System. [PDF]

Med Res Rev
ABSTRACT Cholinergic transmission plays a critical role in both the central and peripheral nervous systems, affecting processes such as learning, memory, and inflammation. Conventional cholinergic drugs generally suffer from poor selectivity and temporal precision, leading to undesired effects and limited therapeutic efficacy. Photopharmacology aims to
Colleoni A, Galli G, Dallanoce C, De Amici M, Gorostiza P, Matera C.   +5 more
europepmc   +2 more sources

The M1 muscarinic acetylcholine receptor subtype is important for retinal neuron survival in aging mice

Scientific Reports, 2019
Muscarinic acetylcholine receptors have been implicated as potential neuroprotective targets for glaucoma. We tested the hypothesis that the lack of a single muscarinic receptor subtype leads to age-dependent neuron reduction in the retinal ganglion cell
Panagiotis Laspas, Mayagozel B. Zhutdieva, Christoph Brochhausen, Aytan Musayeva, Jenia Kouchek Zadeh, Norbert Pfeiffer, Ning Xia, Huige Li, Juergen Wess, Adrian Gericke   +9 more
doaj   +2 more sources

Development of VU6036864: A Triazolopyridine-Based High-Quality Antagonist Tool Compound of the M₅ Muscarinic Acetylcholine Receptor. [PDF]

J Med Chem
While the muscarinic acetylcholine receptor mAChR subtype 5 (M5) has been studied over decades, recent findings suggest that more in-depth research is required to elucidate a thorough understanding of its physiological function related to neurological ...
Li J, Orsi DL, Engers JL, Long MF, Capstick RA, Maurer MA, Presley CC, Vinson PN, Rodriguez AL, Han A, Cho HP, Chang S, Jackson M, Bubser M, Blobaum AL, Boutaud O, Nader MA, Niswender CM, Conn PJ, Jones CK, Lindsley CW, Han C.   +21 more
europepmc   +2 more sources

Synergistic Antiemetic Effects of Nerolidol on Domperidone, Hyoscine, and Ondansetron: In Vivo and in Silico Investigations on Receptor Binding Affinity. [PDF]

ChemistryOpen
Nerolidol shows prominent antiemetic activity and mitigates CuSO4.H2O‐mediated retching in chicks efficiently through its peripheral action. Additionally, the in silico studies have also shown possible antiemetic effects with greater binding affinity against muscarinic (specially, M2 and M3) and dopaminergic receptors.
Ghosh Situ S, Bhuia MS, Chowdhury R, Al Hasan S, Akber Ansari S, Aamer Ansari I, Ali A, Torequl Islam M.   +7 more
europepmc   +2 more sources