Results 21 to 30 of about 15,215 (194)

Xanomeline displays concomitant orthosteric and allosteric binding modes at the M4 mAChR

Nature Communications, 2023
The M4 muscarinic acetylcholine receptor (M4 mAChR) has emerged as a drug target of high therapeutic interest due to its expression in regions of the brain involved in the regulation of psychosis, cognition, and addiction.
Wessel A. C. Burger, Vi Pham, Ziva Vuckovic, Alexander S. Powers, Jesse I. Mobbs, Yianni Laloudakis, Alisa Glukhova, Denise Wootten, Andrew B. Tobin, Patrick M. Sexton, Steven M. Paul, Christian C. Felder, Radostin Danev, Ron O. Dror, Arthur Christopoulos, Celine Valant, David M. Thal   +16 more
doaj   +1 more source

Increased cocaine self-administration in M4 muscarinic acetylcholine receptor knockout mice [PDF]

Psychopharmacology, 2011
The reinforcing effects of cocaine are mediated by the mesolimbic dopamine system. Behavioral and neurochemical studies have shown that the cholinergic muscarinic M(4) receptor subtype plays an important role in regulation of dopaminergic neurotransmission.Here we investigated for the first time the involvement of M(4) receptors in the reinforcing ...
Schmidt, Lene Sørensen, Thomsen, Morgane, Weikop, Pia, Nielsen, Ditte Dencker, Wess, Jürgen, Woldbye, David Paul Drucker, Wörtwein, Gitta, Fink-Jensen, Anders   +7 more
openaire   +3 more sources

The structural study of mutation-induced inactivation of human muscarinic receptor M4

IUCrJ, 2020
Human muscarinic receptor M4 belongs to the class A subfamily of the G-protein-coupled receptors (GPCRs). M4 has emerged as an attractive drug target for the treatment of Alzheimer's disease and schizophrenia.
Jingjing Wang, Meng Wu, Lijie Wu, Yueming Xu, Fei Li, Yiran Wu, Petr Popov, Lin Wang, Fang Bai, Suwen Zhao, Zhi-Jie Liu, Tian Hua   +11 more
doaj   +1 more source

Live-cell microscopy or fluorescence anisotropy with budded baculoviruses—which way to go with measuring ligand binding to M4 muscarinic receptors?

Open Biology, 2022
M4 muscarinic acetylcholine receptor is a G protein-coupled receptor (GPCR) that has been associated with alcohol and cocaine abuse, Alzheimer's disease, and schizophrenia which makes it an interesting drug target.
Maris-Johanna Tahk, Jane Torp, Mohammed A. S. Ali, Dmytro Fishman, Leopold Parts, Lukas Grätz, Christoph Müller, Max Keller, Santa Veiksina, Tõnis Laasfeld, Ago Rinken   +10 more
doaj   +1 more source

Novel Interaction between the M4 Muscarinic Acetylcholine Receptor and Elongation Factor 1A2 [PDF]

Journal of Biological Chemistry, 2002
The activation of the muscarinic acetylcholine receptor (mAChR) family, consisting of five subtypes (M1-M5), produces a variety of physiological effects throughout the central nervous system. However, the role of each individual subtype remains poorly understood.
McClatchy, D.B., Knudsen, C.R., Clark, Brian F. C., Kahn, R.A., Hall, R.A., Levey, A.I.   +5 more
openaire   +3 more sources

Discovery of the First Selective M4 Muscarinic Acetylcholine Receptor Antagonists with in Vivo Antiparkinsonian and Antidystonic Efficacy.

ACS Pharmacology & Translational Science, 2021
Nonselective antagonists of muscarinic acetylcholine receptors (mAChRs) that broadly inhibit all five mAChR subtypes provide an efficacious treatment for some movement disorders, including Parkinson's disease and dystonia. Despite their efficacy in these
M. Moehle, Aaron M. Bender, J. Dickerson, Daniel J. Foster, Aidong Qi, Hyekyung P. Cho, Yuping Donsante, Weimin Peng, Zoey Bryant, Kaylee J Stillwell, T. Bridges, Sichen Chang, Katherine J. Watson, Jordan C. O’Neill, Julie L Engers, Li Peng, Alice L. Rodriguez, C. Niswender, C. Lindsley, E. Hess, P. Conn, J. M. Rook   +21 more
semanticscholar   +1 more source

Structure-function studies of M4 muscarinic acetylcholine receptor allosteric modulation [PDF]

Journal of Biological Chemistry, 2017
The M4 muscarinic acetylcholine receptor (mAChR) is implicated in many central nervous system disorders, however, due to a highly conserved acetylcholine (ACh) binding orthosteric site, there is a lack of highly selective ligands as therapeutics and experimental probes for this target.
Vindhya Nawaratne, Katie Leach, Christian C. Felder, Patrick M. Sexton, Arthur Christopoulos   +4 more
openaire   +2 more sources

Pharmaceutical Assessment Suggests Locomotion Hyperactivity in Zebrafish Triggered by Arecoline Might Be Associated with Multiple Muscarinic Acetylcholine Receptors Activation

Toxins, 2021
Arecoline is one of the nicotinic acid-based alkaloids, which is found in the betel nut. In addition to its function as a muscarinic agonist, arecoline exhibits several adverse effects, such as inducing growth retardation and causing developmental ...
Petrus Siregar, Gilbert Audira, Ling-Yi Feng, Jia-Hau Lee, Fiorency Santoso, Wen-Hao Yu, Yu-Heng Lai, Jih-Heng Li, Ying-Ting Lin, Jung-Ren Chen, Chung-Der Hsiao   +10 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

Discovery of VU6028418: A Highly Selective and Orally Bioavailable M4 Muscarinic Acetylcholine Receptor Antagonist.

ACS Medicinal Chemistry Letters, 2021
Herein, we report the SAR leading to the discovery of VU6028418, a potent M4 mAChR antagonist with high subtype-selectivity and attractive DMPK properties in vitro and in vivo across multiple species. VU6028418 was subsequently evaluated as a preclinical
Matthew Spock, Trever R. Carter, Katrina A. Bollinger, Changho Han, Logan A Baker, Alice L. Rodriguez, Li Peng, J. Dickerson, Aidong Qi, J. M. Rook, Jordan C. O’Neill, Katherine J. Watson, Sichen Chang, T. Bridges, Julie L Engers, D. Engers, C. Niswender, P. Conn, C. Lindsley, Aaron M. Bender   +19 more
semanticscholar   +1 more source