Results 21 to 30 of about 5,131 (212)

Crystal structure of the M₅ muscarinic acetylcholine receptor [PDF]

Proceedings of the National Academy of Sciences, 2019
AbstractThe human M5 muscarinic acetylcholine receptor (mAChR) has recently emerged as an exciting therapeutic target for treating a range of disorders, including drug addiction. However, a lack of structural information for this receptor subtype has limited further drug development and validation.
Patrick M. Sexton, Patrick M. Sexton, Wessel A.C. Burger, Kunio Hirata, Christopher J. Langmead, Raphaël Rahmani, Geoff Thompson, Swapna Varghese, Craig W. Lindsley, Celine Valant, Patrick R. Gentry, Arthur Christopoulos, Jonathan B. Baell, Andrew B. Tobin, David M. Thal, Alice E. Berizzi, Emma T van der Westhuizen, Ziva Vuckovic   +17 more
openaire   +6 more sources

Molecular Mechanisms of Action of M5 Muscarinic Acetylcholine Receptor Allosteric Modulators [PDF]

Molecular Pharmacology, 2016
Recently, the first subtype-selective allosteric modulators of the M5 muscarinic acetylcholine receptor (mAChR) have been described, but their molecular mechanisms of action remain unknown. Using radioligand-binding and functional assays of inositol phosphate (IP) accumulation and Ca(2+) mobilization in a recombinant cell line stably expressing the ...
Sandra Den Hoedt, Alice E. Berizzi, Patrick R. Gentry, Patrick M. Sexton, Christopher J. Langmead, Arthur Christopoulos, Patricia Rueda   +6 more
openaire   +2 more sources

Expression Profiles of Neuropeptides, Neurotransmitters, and Their Receptors in Human Keratocytes In Vitro and In Situ. [PDF]

PLoS ONE, 2015
Keratocytes, the quiescent cells of the corneal stroma, play a crucial role in corneal wound healing. Neuropeptides and neurotransmitters are usually associated with neuronal signaling, but have recently been shown to be produced also by non-neuronal ...
Marta Słoniecka, Sandrine Le Roux, Peter Boman, Berit Byström, Qingjun Zhou, Patrik Danielson   +5 more
doaj   +1 more source

Long-Term—But Not Short-Term—Plasticity at the Mossy Fiber–CA3 Pyramidal Cell Synapse in Hippocampus Is Altered in M1/M3 Muscarinic Acetylcholine Receptor Double Knockout Mice

Cells, 2023
Muscarinic acetylcholine receptors are well-known for their crucial involvement in hippocampus-dependent learning and memory, but the exact roles of the various receptor subtypes (M1–M5) are still not fully understood.
Fang Zheng, Jürgen Wess, Christian Alzheimer   +2 more
doaj   +1 more source

Intestinal epithelial stem/progenitor cells are controlled by mucosal afferent nerves. [PDF]

PLoS ONE, 2011
BACKGROUND: The maintenance of the intestinal epithelium is of great importance for the survival of the organism. A possible nervous control of epithelial cell renewal was studied in rats and mice.
Ove Lundgren, Mats Jodal, Madeleine Jansson, Anders T Ryberg, Lennart Svensson   +4 more
doaj   +1 more source

Fine Tuning Muscarinic Acetylcholine Receptor Signaling Through Allostery and Bias

Frontiers in Pharmacology, 2021
The M1 and M4 muscarinic acetylcholine receptors (mAChRs) are highly pursued drug targets for neurological diseases, in particular for Alzheimer’s disease and schizophrenia.
Emma T. van der Westhuizen, K. H. Christopher Choy, Celine Valant, Simon McKenzie-Nickson, Sophie J. Bradley, Andrew B. Tobin, Patrick M. Sexton, Arthur Christopoulos   +7 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

Acetylcholine and spinal locomotor networks: The insider

Physiological Reports, 2021
This article aims to review studies that have investigated the role of neurons that use the transmitter acetylcholine (ACh) in controlling the operation of locomotor neural networks within the spinal cord. This cholinergic system has the particularity of
Théo Mille, Camille Quilgars, Jean‐René Cazalets, Sandrine S. Bertrand   +3 more
doaj   +1 more source

Assessment of Quercetin Antiemetic Properties: In Vivo and In Silico Investigations on Receptor Binding Affinity and Synergistic Effects

Plants, 2023
Quercetin (QUA), a flavonoid compound, is ubiquitously found in plants and has demonstrated a diverse range of biological activities. The primary objective of the current study is to assess the potential antiemetic properties of QUA using an in vivo and ...
Raihan Chowdhury, Md. Shimul Bhuia, Asraful Islam Rakib, Rubel Hasan, Henrique Douglas Melo Coutinho, Isaac Moura Araújo, Irwin Rose Alencar de Menezes, Muhammad Torequl Islam   +7 more
doaj   +1 more source

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