Results 41 to 50 of about 29,153 (282)

Novel Fused Arylpyrimidinone Based Allosteric Modulators of the M1 Muscarinic Acetylcholine Receptor. [PDF]

ACS Chemical Neuroscience, 2016
Benzoquinazolinone 1 is a positive allosteric modulator (PAM) of the M1 muscarinic acetylcholine receptor (mAChR), which is significantly more potent than the prototypical PAM, 1-(4-methoxybenzyl)-4-oxo-1,4-dihydroquinoline- 3-carboxylic acid (BQCA). In
Shailesh N Mistry, H. Lim, M. Jörg, B. Capuano, A. Christopoulos, J. R. Lane, P. Scammells   +6 more
semanticscholar   +4 more sources

[11C]AF150(S), an agonist PET ligand for M1 muscarinic acetylcholine receptors [PDF]

EJNMMI Research, 2013
The M1 muscarinic acetylcholine receptor (M1ACh-R) is a G protein-coupled receptor that can occur in interconvertible coupled and uncoupled states. It is enriched in the basal ganglia, hippocampus, olfactory bulb, and cortical areas, and plays a role in motor and cognitive functions. Muscarinic M1 agonists are potential therapeutic agents for cognitive
Buiter, H.J.C., Windhorst, A.D., Huisman, M.C., Yaqub, M.M., Knol, D.L., Fisher, A., Lammertsma, A.A., Leysen, J.E.   +7 more
openaire   +4 more sources

Histamine H1 Receptor Down-Regulation Mediated by M3 Muscarinic Acetylcholine Receptor Subtype

Journal of Pharmacological Sciences, 2004
Heterologous down-regulation of histamine H1 receptor (H1R) mediated by muscarinic acetylcholine receptor subtype was investigated using five kinds of Chinese hamster ovary (CHO) cells stably co-expressing the human H1R and one of the five (M1 –M5 ...
Katsuhiro Miyoshi, Nozomi Kawakami, Yousuke Wakayama, Norimasa Izumi, Shuhei Horio, Hiroyuki Fukui   +5 more
doaj   +1 more source

The effects of kindling during pregnancy on long-term potentiation (LTP) induction and M1 muscarinic acetylcholine receptors in male rat offspring

Research in Pharmaceutical Sciences, 2023
Background and purpose: Neonates of pregnant women with epilepsy may compromise normal neurodevelopment and hippocampal morphology. Memory and learning disorders and a decrease in verbal IQ scores are seen in these children later in life. In the previous
Ali Pourmotabbed, Razieh Naghizadeh, Farshad Moradpour, Mozhgan Veisi, Seyed Ershad Nedaei, Fatemeh Zarei, Zahra Salimi   +6 more
doaj   +1 more source

An in vivo biosensor for neurotransmitter release and in situ receptor activity. [PDF]

, 2010
Tools from molecular biology, combined with in vivo optical imaging techniques, provide new mechanisms for noninvasively observing brain processes. Current approaches primarily probe cell-based variables, such as cytosolic calcium or membrane potential ...
Griesbeck, Oliver, Kleinfeld, David, Mank, Marco, Muller, Arnaud, Nguyen, Quoc-Thang, Schroeder, Lee F, Taylor, Palmer   +6 more
core   +2 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

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

, 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.
Arthur Christopoulos, Aurelio L., Avlani V. A., Barbosa J., Bell R. P., Ben Capuano, Bunce R. A., Canals M., Cao X., Casara P., Celine Valant, Conn P. J., Decker M., Eaton P. E., Gould R. G., Holden M., Koguro K., Kuduk S. D., Kuduk S. D., Kuduk S. D., Kuduk S. D., Kuduk S. D., Kuduk S. D., Kuduk S. D., Kuduk S. D., Langmead C. J., Lauer W. M., Leach K., Ma L., Maffioli S. I., Meanwell N. A., Medeiros R. R., Patrick M. Sexton, Peter J. Scammells, Podányi B., Reid P. R., Shailesh N. Mistry, Shirey J. K., Wess J., Wise W. M., Yang F. V., Zewge D., Zhang Y., Škugor M. M.   +43 more
core   +2 more sources

Muscarinic acetylcholine M1 receptor regulates pyroptosis of prostate cancer cells through Caspase-1/GSDMD pathway

Di-san junyi daxue xuebao, 2021
Objective To determine the effect of muscarinic acetylcholine M1 receptor (CHRM1) on pyroptosis of prostate cancer cells and investigate its possible molecular mechanism. Methods Pirenzepine (PIN), a specific CHRM1 antagonist, and bethanechol (BETH), its
CHEN Jinying, ZHANG Mi, ZENG Yan, HUANG Yanping, CHEN Fangfang, WANG Qianhui, XU Chen   +6 more
doaj   +1 more source

The M1 muscarinic acetylcholine receptor in the crypt stem cell compartment mediates intestinal mucosal growth

Experimental biology and medicine, 2020
Maintenance of the highly plastic intestinal epithelium relies upon stem cells localized to intestinal crypts. Recent evidence suggests muscarinic acetylcholine signaling impacts epithelial barrier function, proliferation, and apoptosis.
Chasen J Greig, Sarah J. Armenia, R. Cowles   +2 more
semanticscholar   +1 more source

Carbachol Induces Ca2+-Dependent Contraction via Muscarinic M2 and M3 Receptors in Rat Intestinal Subepithelial Myofibroblasts

Journal of Pharmacological Sciences, 2009
.: Intestinal myofibroblasts (IMFs) that exist adjacent to the basement membrane of intestines have contractility and contribute to physical barriers of the intestine.
Koichi Iwanaga, Takahisa Murata, Muneyoshi Okada, Masatoshi Hori, Hiroshi Ozaki   +4 more
doaj   +1 more source