Results 41 to 50 of about 15,215 (194)

Discovery of Pre-Clinical Candidate <b>VU6008055</b>/<b>AF98943</b>: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic M₄ Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM) with Robust In Vivo Efficacy. [PDF]

ACS Chem Neurosci
Herein, we report the structure–activity relationship to develop novel tricyclic M4 positive allosteric modulator scaffolds with improved pharmacological properties.
Engers JL, Bollinger SR, Gregro AR, Capstick RA, Spearing PK, Long MF, Tarr JC, Watson KJ, Chang S, Luscombe VB, Rodriguez AL, Cho HP, Qi A, Niswender CM, Bubser M, Gould RW, Robb WH, Byun N, Gore J, Jones CK, Thomsen MS, Bridges TM, Boutaud O, Conn PJ, Engers DW, Lindsley CW, Temple KJ.   +26 more
europepmc   +2 more sources

[¹¹C]MK-6884 PET imaging reveals lower M₄ muscarinic acetylcholine receptor availability following cocaine self-administration in male rats. [PDF]

Pharmacol Rep
Cocaine Use Disorder (CUD) remains a significant problem in the United States, with high rates of relapse and no present FDA-approved treatment. The acetylcholine neurotransmitter system, specifically through modulation of muscarinic acetylcholine ...
Gollapelli KK, Krizan I, Bhoopal B, Damuka N, Moriarty C, Miller M, Sai KKS, Gould RW.   +7 more
europepmc   +2 more sources

Functional Activation of G-Proteins Coupled With Muscarinic Acetylcholine Receptors in Rat Brain Membranes

Journal of Pharmacological Sciences, 2014
.: The functional activation of Gi/o proteins coupled to muscarinic acetylcholine receptors (mAChRs) was investigated with the conventional guanosine-5′-O-(3-[35S]thio)triphosphate ([35S]GTPγS) binding assay in rat brain membranes.
Yuji Odagaki, Masakazu Kinoshita, Ryoichi Toyoshima   +2 more
doaj   +1 more source

The Muscarinic Acetylcholine Receptor Agonist BuTAC Mediates Antipsychotic-Like Effects via the M4 Subtype [PDF]

Neuropsychopharmacology, 2013
The generation of muscarinic acetylcholine receptor (mAChR) subtype-selective compounds has been challenging, requiring use of nonpharmacological approaches, such as genetically engineered animals, to deepen our understanding of the potential that members of the muscarinic receptor subtype family hold as therapeutic drug targets.
Marla L, Watt, Linda, Rorick-Kehn, David B, Shaw, Karen M, Knitowski, Anne T, Quets, Amy K, Chesterfield, David L, McKinzie, Christian C, Felder   +7 more
openaire   +2 more sources

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

Muscarinic Receptor Subtypes Mediating Positive and Negative Inotropy in the Developing Chick Ventricle

Journal of Pharmacological Sciences, 2007
The inotropic response to muscarinic receptor stimulation of isolated chick ventricular myocardium was examined at various developmental stages, and the receptor subtype involved was pharmacologically characterized.
Hideaki Nouchi, Seri Kaeriyama, Akiko Muramatsu, Masumi Sato, Kunihiko Hirose, Nagako Shimizu, Hikaru Tanaka, Koki Shigenobu   +7 more
doaj   +1 more source

Long-term activation upon brief exposure to xanomleline is unique to M1 and M4 subtypes of muscarinic acetylcholine receptors. [PDF]

PLoS ONE, 2014
Xanomeline is an agonist endowed with functional preference for M1/M4 muscarinic acetylcholine receptors. It also exhibits both reversible and wash-resistant binding to and activation of these receptors.
Eva Šantrůčková, Vladimír Doležal, Esam E El-Fakahany, Jan Jakubík   +3 more
doaj   +1 more source

Characterization of a Novel M4 PAM PET Radioligand [11C]PF06885190 in Nonhuman Primates (NHP)

Molecules, 2023
Muscarinic acetylcholine receptors (mAChR), including M4, draw attention as therapeutic targets for several neurodegenerative diseases including Alzheimer’s disease (AD).
Sangram Nag, Ryosuke Arakawa, Zhisheng Jia, Erik Lachapelle, Lei Zhang, Kevin Maresca, Laigao Chen, Mahabuba Jahan, Timothy Mccarthy, Christer Halldin   +9 more
doaj   +1 more source

Stimulation of the muscarinic receptor M4 regulates neural precursor cell proliferation and promotes adult hippocampal neurogenesis

Development, 2023
Cholinergic signaling plays a crucial role in the regulation of adult hippocampal neurogenesis; however, the mechanisms by which acetylcholine mediates neurogenic effects are not completely understood.
Lidia I. Madrid, Katelyn Hafey, Saurabh Bandhavkar, Gabriela O Bodea, Javier Jimenez-Martin, Michael Milne, Tara L Walker, G. Faulkner, Elizabeth J Coulson, D. Jhaveri   +9 more
semanticscholar   +1 more source

Cell-Type Specific Neuromodulation of Excitatory and Inhibitory Neurons via Muscarinic Acetylcholine Receptors in Layer 4 of Rat Barrel Cortex

Frontiers in Neural Circuits, 2022
The neuromodulator acetylcholine (ACh) plays an important role in arousal, attention, vigilance, learning and memory. ACh is released during different behavioural states and affects the brain microcircuit by regulating neuronal and synaptic properties ...
Guanxiao Qi, Dirk Feldmeyer, Dirk Feldmeyer, Dirk Feldmeyer   +3 more
doaj   +1 more source