Results 11 to 20 of about 13,945 (210)

Dualsteric modulators of the M2 muscarinic acetylcholine receptor [PDF]

Journal of Cheminformatics, 2014
G-protein coupled receptors (GPCRs) trigger multiple signal-switching mechanisms like binding of s-arrestin proteins, activation of kinases and G-protein activation [1]. The poor understanding of the conformational changes resulting in these activations is a major challenge for the design of specific GPCR modulating drugs.
Marcel Bermudez, Gerhard Wolber
openaire   +1 more source

Sodium ions allosterically modulate the M2 muscarinic receptor [PDF]

Scientific Reports, 2020
AbstractG protein coupled receptors (GPCRs) play a key role in the vast majority of cellular signal transduction processes. Previous experimental evidence has shown that sodium ion (Na+) allosterically modulate several class A GPCRs and theoretical studies suggested that the same also holds true for muscarinic receptors. Here we examined, using Xenopus
Friedman, Sheli, Tauber, Merav, Ben-Chaim, Yair   +2 more
openaire   +2 more sources

Eosinophil-mediated cholinergic nerve remodeling [PDF]

, 2006
Eosinophils are observed to localize to cholinergic nerves in a variety of inflammatory conditions such as asthma, rhinitis, eosinophilic gastroenteritis, and inflammatory bowel disease, where they are also responsible for the induction of cell ...
McLean, W.G., Anthony G. Fenech, Madziar, B., Madziar, Beata, Durcan, Niamh, Gleich, G.J., Walsh, M., Fenech, Anthony G., McLean, Graham W., Jan Blusztajn, Gerard J. Gleich, Gleich, Gerard J., Niamh Durcan, Hall, Ian P., Beata Madziar, Walsh, Marie-Therese, Hall, I.P., Ian P. Hall, Durcan, N., Costello, Richard W., Richard W. Costello, Marie-Therese Walsh, McGarvey, Lorcan, Costello, R.W., Fenech, A.G., W. Graham McLean, Lorcan McGarvey, Blusztain, J., Blusztajn, Jan   +28 more
core   +1 more source

Antipsychotic-like effect of the muscarinic acetylcholine receptor agonist BuTAC in non-human primates. [PDF]

PLoS ONE, 2015
Cholinergic, muscarinic receptor agonists exhibit functional dopamine antagonism and muscarinic receptors have been suggested as possible future targets for the treatment of schizophrenia and drug abuse. The muscarinic ligand (5R,6R)-6-(3-butylthio-1,2,5-
Maibritt B Andersen, Carrie Hughes Croy, Ditte Dencker, Thomas Werge, Frank P Bymaster, Christian C Felder, Anders Fink-Jensen   +6 more
doaj   +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

Organophosphorus pesticides decrease M2 muscarinic receptor function in guinea pig airway nerves via indirect mechanisms. [PDF]

PLoS ONE, 2010
Epidemiological studies link organophosphorus pesticide (OP) exposures to asthma, and we have shown that the OPs chlorpyrifos, diazinon and parathion cause airway hyperreactivity in guinea pigs 24 hr after a single subcutaneous injection.
Becky J Proskocil, Donald A Bruun, Charles M Thompson, Allison D Fryer, Pamela J Lein   +4 more
doaj   +1 more source

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

Increased expression of neuregulin 1 in the urothelium of rat bladder with partial bladder outlet obstruction

BMC Urology, 2017
Background This study determined whether changes in the expression of neuregulin (NRG) 1, erbB2 tyrosine kinase (ErbB2) and the M2 muscarinic receptor in the urothelium and detrusor muscle of the rat bladder were associated with partial bladder outlet ...
Seung Woo Yang, Seong Woo Jeong, Ki Hak Song   +2 more
doaj   +1 more source

Effects of tetrahydroaminoacridine on M1 and M2 muscarine receptors

Neuroscience Letters, 1988
Tetrahydroaminoacridine (THA) has been reported to improve the memory of persons with Alzheimer's disease, but its mechanism of action is uncertain. We found that clinically effective concentrations, 0.03-0.3 microM, readily inhibit acetylcholinesterase and butyrylcholinesterase from rabbit hippocampal tissue in artificial cerebrospinal fluid (CSF) at ...
B D, Pearce, L T, Potter
openaire   +2 more sources

Muscarinic cholinergic receptor (M2) plays a crucial role in the development of myopia in mice

Disease Models & Mechanisms, 2013
SUMMARY Myopia is a huge public health problem worldwide, reaching the highest incidence in Asia. Identification of susceptible genes is crucial for understanding the biological basis of myopia.
Veluchamy A. Barathi, Jia Lin Kwan, Queenie S. W. Tan, Sung Rhan Weon, Li Fong Seet, Liang Kee Goh, Eranga N. Vithana, Roger W. Beuerman   +7 more
doaj   +1 more source