Identification of Candidate Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor Which May Improve Vagus Nerve Stimulation in Chronic Tinnitus [PDF]
Chronic tinnitus is characterized by neuroplastic changes of the auditory cortex. A promising method for therapy of chronic tinnitus is vagus nerve stimulation (VNS) combined with auditory stimulation.
Tijana Bojić+3 more
openalex +2 more sources
Structures of the M1 and M2 muscarinic acetylcholine receptor/G-protein complexes [PDF]
Choosing a partner G protein–coupled receptors (GPCRs) bind ligands outside the cell and trigger events inside the cell by selectively binding and activating specific G proteins. The selectivity occurs even among highly related GPCRs.
S. Maeda+4 more
semanticscholar +4 more sources
Evaluation of the Alterations in Central Cholinergic Neurotransmission in Aging and Amyloid Precursor Protein Knock-In Mice. [PDF]
In Alzheimer's disease, reduced release of ACh is linked more to Aβ pathology than to age‐related change, highlighting an early sign of disease. ABSTRACT A progressive decline in cognitive function occurs as a result of aging and Alzheimer's disease (AD) and is primarily associated with diminished cholinergic neurotransmission.
Nagai-Arakawa I+14 more
europepmc +2 more sources
Light-Activated Pharmacological Tools for Exploring the Cholinergic System. [PDF]
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+5 more
europepmc +2 more sources
Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias
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+7 more
doaj +2 more sources
Activation of Muscarinic M1 Acetylcholine Receptors Induces Long-Term Potentiation in the Hippocampus [PDF]
Muscarinic M1 acetylcholine receptors (M1Rs) are highly expressed in the hippocampus, and their inhibition or ablation disrupts the encoding of spatial memory.
Broad, Lisa M+9 more
core +7 more sources
Allosteric Modulation of M1 Muscarinic Acetylcholine Receptor Internalization and Subcellular Trafficking* [PDF]
Background: The effects of allosteric modulators on G protein-coupled receptor trafficking are largely unknown. Results: The allosteric ligand BQCA modulates M1 mAChR arrestin recruitment and receptor trafficking.
Holly R. Yeatman+6 more
semanticscholar +4 more sources
Structure of the m1 Muscarinic Acetylcholine Receptor Gene and Its Promoter [PDF]
The m1 receptor is one of five muscarinic receptors that mediate the metabotropic actions of acetylcholine in the nervous system where it is expressed predominantly in the telencephalon and autonomic ganglia. RNase protection, primer extension, and 5'-rapid amplification of cDNA ends analysis of a rat cosmid clone containing the entire m1 gene ...
S. Pepitoni, Noel J. Buckley, Ian Wood
openalex +5 more sources
Corrigendum: Striatal dopamine D2-muscarinic acetylcholine M1 receptor-receptor interaction in a model of movement disorders [PDF]
René A. J. Crans+13 more
doaj +2 more sources
Single nucleotide polymorphisms of the human M1 muscarinic acetylcholine receptor gene [PDF]
The gene encoding the human muscarinic receptor, type 1 (CHRM1), was genotyped from 245 samples of the Coriell Collection (Coriell Institute for Medical Research, Camden, NJ). Fifteen single nucleotide polymorphisms (SNPs) were discovered, 9 of which are located in the coding region of the receptor.
Julie L. Lucas+2 more
openalex +4 more sources