Results 21 to 30 of about 22,337 (268)

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

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

Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]

, 2018
The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

Vitamin E can compensate the density of M1 receptors in the hippocampus of scopolamine-treated rats

Folia Neuropathologica, 2018
M1 muscarinic receptor plays a fundamental role in memory and is closely associated with Alzheimer’s disease (AD); it has long been assumed as a therapeutic goal. By activating of the cholinergic receptor vitamin E helps with memory retention.
Ali Sayyahi, Mehrdad Jahanshahi, Hossein Amini, Hamid Sepehri   +3 more
doaj   +1 more source

The Spinal Muscarinic M1 Receptors and GABAA Receptors Contribute to the McN-A-343–Induced Antinociceptive Effects During Thermal Stimulation of Mice

Journal of Pharmacological Sciences, 2008
The present study was undertaken to clarify how spinal muscarinic receptors are involved in the antinociceptive effects in thermal stimulation. Intrathecal (i.t.) injection of the muscarinic agonist McN-A-343 inhibited the tail-flick response to noxious ...
Kenji Honda, Keigo Horikawa, Suguru Ando, Kohei Koga, Satoshi Kawata, Keisuke Migita, Yukio Takano   +6 more
doaj   +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

Agonist-induced desensitization and phosphorylation of m1-muscarinic receptors [PDF]

Biochemical Journal, 1999
Pre-stimulation of Chinese hamster ovary (CHO) cells expressing the human m1-muscarinic receptor (CHO-m1 cells) with a maximally effective concentration of the muscarinic agonist methacholine resulted in desensitization of Ins(1,4,5)P3 accumulation, apparent as a ∼ 4-fold shift in the agonist dose–response curve.
Waugh, MG, John Challiss RA, Berstein, G, Nahorski, SR, Tobin, AB   +4 more
openaire   +5 more sources

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 ...
Bradley D. Pearce, Lincoln T. Potter
openaire   +3 more sources

A Cholinergic Synaptically Triggered Event Participates in the Generation of Persistent Activity Necessary for Eye Fixation [PDF]

, 2004
An exciting topic regarding integrative properties of the nervous system is how transient motor commands or brief sensory stimuli are able to evoke persistent neuronal changes, mainly as a sustained, tonic action potential firing.
Alvarado, Juan Carlos, Delgado García, José María, Escudero González, Miguel, Márquez Ruiz, Javier, Navarro López, Juan de Dios, Yajeya, Javier   +5 more
core   +4 more sources

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 ...
David A. Evans, Bingfa Sun, Mark G. Bures, Arthur Christopoulos, William I. Weis, Vindhya Nawaratne, Brian K. Kobilka, Katie Leach, Dan Feng, Patrick M. Sexton, Christian C. Felder, Tong Sun Kobilka, Priti Bachhawat, David M. Thal   +13 more
openaire   +3 more sources