Flavonoids with M1 Muscarinic Acetylcholine Receptor Binding Activity [PDF]
Muscarinic acetylcholine receptor-active compounds have potential for the treatment of Alzheimer’s disease. In this study, a series of natural and synthetic flavones and flavonols was assayed in vitro for their ability to inhibit radioligand binding at ...
Meyyammai Swaminathan +6 more
doaj +3 more sources
Enhancing remyelination in multiple sclerosis via M1 muscarinic acetylcholine receptor. [PDF]
Multiple sclerosis (MS) is growing in prevalence; yet, treatments that can reverse the progression of the disease are still needed. One strategy that has shown promise for reversing MS is remyelination by inhibiting the M1 receptor, a member of the muscarinic acetylcholine receptor (mAChR) family.
Chen K, Park E, Abd-Elrahman KS.
europepmc +5 more sources
M1 muscarinic acetylcholine receptor dysfunction in moderate Alzheimer’s disease pathology [PDF]
AbstractAggregation of amyloid beta and loss of cholinergic innervation in the brain are predominant components of Alzheimer’s disease pathology and likely underlie cognitive impairment. Acetylcholinesterase inhibitors are one of the few treatment options for Alzheimer’s disease, where levels of available acetylcholine are enhanced to counteract the ...
Jee Hyun Yi +6 more
openalex +5 more sources
Muscarinic acetylcholine receptor M1 (CHRM1; HM1) [PDF]
openalex +3 more sources
Mechanistic insights into allosteric structure-function relationships at the M1 muscarinic acetylcholine receptor [PDF]
Background: Selective and potent positive allosteric modulators (PAMs) of the M1 mAChR have been recently described. Results: Use of structural analogues and mutagenic mapping identified the mechanistic basis for increased PAM activity.
Abdul-Ridha +42 more
core +7 more sources
Allosteric Modulation of M1 Muscarinic Acetylcholine Receptor Internalization and Subcellular Trafficking [PDF]
Allosteric modulators are an attractive approach to achieve receptor subtype-selective targeting of G protein-coupled receptors. Benzyl quinolone carboxylic acid (BQCA) is an unprecedented example of a highly selective positive allosteric modulator of the M1 muscarinic acetylcholine receptor (mAChR).
Holly R. Yeatman +6 more
openalex +4 more sources
Targeting the M1 muscarinic acetylcholine receptor in Alzheimer’s disease [PDF]
Abstract Alzheimer’s disease (AD) remains a major cause of morbidity and mortality worldwide, and despite extensive research, only a few drugs are available for management of the disease. One strategy has been to up-regulate cholinergic neurotransmission to improve cognitive function, but this approach has dose-limiting adverse effects ...
Louis Dwomoh +2 more
openalex +4 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
Adrenergic receptor β2 (ADRB2); ADRB3; muscarinic acetylcholine receptor M1 (CHRM1; HM1) [PDF]
openalex +3 more sources
Muscarinic acetylcholine receptor M1 mutations causing neurodevelopmental disorder and epilepsy [PDF]
De novo rare damaging variants in genes involved in critical developmental pathways, notably regulation of synaptic transmission, have emerged as a frequent cause of neurodevelopmental disorders (NDD). NDD show great locus heterogeneity and for many of the associated genes, there is substantial phenotypic diversity, including epilepsy, intellectual ...
Anna Marcé‐Grau +7 more
openaire +5 more sources

