Results 11 to 20 of about 58,465 (248)

Dynamic Regulation of Quaternary Organization of the M1 Muscarinic Receptor by Subtype-selective Antagonist Drugs* [PDF]

Journal of Biological Chemistry, 2016
Although rhodopsin-like G protein-coupled receptors can exist as both monomers and non-covalently associated dimers/oligomers, the steady-state proportion of each form and whether this is regulated by receptor ligands are unknown. Herein we address these
J. Pediani, R. Ward, A. Godin, Sara Marsango, G. Milligan   +4 more
semanticscholar   +3 more sources

M1 muscarinic receptor activation mediates cell death in M1-HEK293 cells. [PDF]

PLoS ONE, 2013
HEK293 cells have been used extensively to generate stable cell lines to study G protein-coupled receptors, such as muscarinic acetylcholine receptors (mAChRs).
E Scott Graham, Kerhan K Woo, Miranda Aalderink, Sandie Fry, Jeffrey M Greenwood, Michelle Glass, Mike Dragunow   +6 more
doaj   +5 more sources

Synthesis and pharmacological profiling of analogues of benzyl quinolone carboxylic acid (BQCA) as allosteric modulators of the M1 muscarinic receptor. [PDF]

Journal of Medicinal Chemistry, 2013
Established therapy in Alzheimer's disease involves potentiation of the endogenous orthosteric ligand, acetylcholine, at the M1 muscarinic receptors found in higher concentrations in the cortex and hippocampus.
Shailesh N Mistry, C. Valant, P. Sexton, B. Capuano, A. Christopoulos, P. Scammells   +5 more
semanticscholar   +4 more sources

Mechanistic Insights into Allosteric Structure-Function Relationships at the M1 Muscarinic Acetylcholine Receptor* [PDF]

Journal of Biological Chemistry, 2014
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.
Alaa Abdul-Ridha, J. R. Lane, Shailesh N Mistry, Laura Lopez, P. Sexton, P. Scammells, A. Christopoulos, Meritxell Canals   +7 more
semanticscholar   +4 more sources

M1 muscarinic acetylcholine receptor in Alzheimer’s disease [PDF]

Neuroscience Bulletin, 2014
The degeneration of cholinergic neurons and cholinergic hypofunction are pathologies associated with Alzheimer's disease (AD). Muscarinic acetylcholine receptors (mAChRs) mediate acetylcholine-induced neurotransmission and five mAChR subtypes (M1-M5) have been identified.
Shangtong Jiang, Yanfang Li, Cuilin Zhang, Yingjun Zhao, G. Bu, Huaxi Xu, Yun-wu Zhang   +6 more
semanticscholar   +4 more sources

First-in-Human Assessment of 11C-LSN3172176, an M1 Muscarinic Acetylcholine Receptor PET Radiotracer

Journal of Nuclear Medicine, 2020
Visual Abstract This was a first-in-human study of the PET radiotracer 11C-LSN3172176 for the muscarinic acetylcholine receptor subtype M1. The objectives of the study were to determine the appropriate kinetic model to quantify binding of the tracer to ...
M. Naganawa, N. Nabulsi, S. Henry, D. Matuskey, Shu-Fei Lin, L. Slieker, A. Schwarz, Nancy Kant, C. Jesudason, K. Ruley, Antonio Navarro, Hong Gao, J. Ropchan, D. Labaree, R. Carson, Yiyun Huang   +15 more
semanticscholar   +1 more source

M1 muscarinic acetylcholine receptor dysfunction in moderate Alzheimer’s disease pathology

Brain Communications, 2020
Aggregation of amyloid beta and loss of cholinergic innervation in the brain are predominant components of Alzheimer’s disease pathology and likely underlie cognitive impairment.
J. Yi, Daniel J. Whitcomb, Se Jin Park, Celia Martinez-Perez, S. Barbati, Scott J Mitchell, Kwangwook Cho   +6 more
semanticscholar   +1 more source

Crystal structures of the M1 and M4 muscarinic acetylcholine receptors [PDF]

Nature, 2016
Muscarinic M1-M5 acetylcholine receptors are G-protein-coupled receptors that regulate many vital functions of the central and peripheral nervous systems. In particular, the M1 and M4 receptor subtypes have emerged as attractive drug targets for treatments of neurological disorders, such as Alzheimer's disease and schizophrenia, but the high ...
D. Thal, Bingfa Sun, D. Feng, Vindhya Nawaratne, K. Leach, C. Felder, M. Bures, David A. Evans, W. Weis, P. Bachhawat, T. S. Kobilka, P. Sexton, B. Kobilka, A. Christopoulos   +13 more
semanticscholar   +4 more sources

Characterization of the positive and negative inotropic effects of acetylcholine in the human myocardium [PDF]

, 1995
In the human isolated myocardium, acetylcholine (10−9 to 10−3 M) elicited a biphasic inotropic effect (a decrease in the lower and an increase in the higher concentration range) in atrial and a positive inotropic effect in ventricular trabeculae. However,
Bos, E. (Egbert), Du, X.Y. (Xiaoyi), Saxena, P.R. (Pramod Ranjan), Schoemaker, R.G. (Regien)   +3 more
core   +7 more sources

Purification and properties of m1-toxin, a specific antagonist of m1 muscarinic receptors [PDF]

The Journal of Neuroscience, 1993
The venom of the Eastern green mamba from Africa, Dendroaspis angusticeps, was found to block the binding of 3H-quinuclidinyl benzilate to pure m1 and m4 muscarinic ACh receptors expressed in Chinese hamster ovary cells. The principal toxin in the venom with anti- m1 muscarinic activity was purified by gel filtration and reversed- phase HPLC.
L. T. Potter, S. I. Max, Jing-Sheng Liang   +2 more
openaire   +3 more sources