Results 151 to 160 of about 15,215 (194)

Thiochrome Enhances Acetylcholine Affinity at Muscarinic M4 Receptors: Receptor Subtype Selectivity via Cooperativity Rather than Affinity

Molecular Pharmacology, 2004
Thiochrome (2,7-dimethyl-5H-thiachromine-8-ethanol), an oxidation product and metabolite of thiamine, has little effect on the equilibrium binding of l-[3H]N-methyl scopolamine ([3H]NMS) to the five human muscarinic receptor subtypes (M1-M5) at concentrations up to 0.3 mM.
S, Lazareno, V, Dolezal, A, Popham, N J M, Birdsall   +3 more
openaire   +2 more sources

Discovery of VU6016235: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM)

ACS Chemical Neuroscience
Herein, we report structure–activity relationship (SAR) studies to develop novel tricyclic M4 PAM scaffolds with improved pharmacological properties. This endeavor involved a “tie-back” strategy to replace a 5-amino-2,4-dimethylthieno[2,3-d]pyrimidine-6 ...
Julie L Engers, Logan A Baker, Sichen Chang, Vincent B Luscombe, Alice L. Rodriguez, C. Niswender, Hyekyung P. Cho, M. Bubser, Analisa Thompson Gray, Carrie K Jones, Weimin Peng, J. M. Rook, T. Bridges, Olivier Boutaud, P. J. Conn, D. Engers, C. Lindsley, Kayla J Temple   +17 more
semanticscholar   +1 more source

PET imaging of M4 muscarinic acetylcholine receptors in rhesus macaques using [11C]MK-6884: Quantification with kinetic modeling and receptor occupancy by CVL-231 (emraclidine), a novel positive allosteric modulator

Journal of Cerebral Blood Flow and Metabolism
Stimulation of the M4 muscarinic acetylcholine receptor reduces striatal hyperdopaminergia, suggesting its potential as a therapeutic target for schizophrenia.
Vasily Belov, N. Guehl, Sridhar Duvvuri, Philip Iredale, Sung-Hyun Moon, M. Dhaynaut, Srinivas Chakilam, Alexander C. MacDonagh, Peter A Rice, Daniel L. Yokell, John J. Renger, G. El Fakhri, M. Normandin   +12 more
semanticscholar   +1 more source

Striatal, Hippocampal, and Cortical Networks Are Differentially Responsive to the M4- and M1-Muscarinic Acetylcholine Receptor Mediated Effects of Xanomeline.

ACS Chemical Neuroscience, 2018
Preclinical and clinical data suggest that muscarinic acetylcholine receptor activation may be therapeutically beneficial for the treatment of schizophrenia and Alzheimer's diseases.
C. Thorn, Joshua Moon, Clinton A Bourbonais, J. Harms, J. Edgerton, Eda Stark, Stefanus J. Steyn, Christopher R Butter, J. Lazzaro, Rebecca E O'connor, M. Popiolek   +10 more
semanticscholar   +1 more source

M4 Muscarinic Acetylcholine Receptor Modulation of Dopamine Receptor Functions

2017
M4 muscarinic acetylcholine receptors (mAChRs) belong to the Rhodopsin family of G protein-couple receptors. These receptors are found most abundantly in the striatum and are implicated in a number of central nervous system disorders, including schizophrenia.
openaire   +1 more source

In Vivo Modulation of Hippocampal Excitability by M4 Muscarinic Acetylcholine Receptor Activator: Implications for Treatment of Alzheimer's Disease and Schizophrenic Patients.

ACS Chemical Neuroscience, 2018
Abnormal hippocampal activity has been linked to impaired cognitive performance in Alzheimer's disease and schizophrenia, leading to a hypothesis that normalization of this activity may be therapeutically beneficial.
M. Popiolek, Y. Mandelblat-Cerf, D. Young, Jonathan Garst-Orozco, S. Lotarski, Eda Stark, Melissa Kramer, Christopher R Butler, R. Kozak   +8 more
semanticscholar   +1 more source

Interaction of anandamide with the M1 and M4 muscarinic acetylcholine receptors

Brain Research, 2001
The M(1) and M(4) muscarinic acetylcholine receptors are the most abundant muscarinic receptor subtypes in the brain, and are involved in learning and memory. Because cannabinoid receptors are also abundantly expressed in similar brain regions and mediate opposite effects to acetylcholine on cognition, the present study investigated whether the ...
A, Christopoulos, K, Wilson
openaire   +2 more sources

Structure-activity relationship of pyrazol-4-yl-pyridine derivatives for imaging the muscarinic acetylcholine receptor M4

Nuclear Medicine and Biology, 2022
Ahmed Haider, Xiaoyun Deng, Stefanie K. Pfister, Troels E Jeppesen, Xia Zhiwei, Jian Rong, T. Connors, T. Collier, L. Mu, R. Schibli, A. Christopoulos, C. Valant, Steven H. Liang   +12 more
semanticscholar   +1 more source

Expression of m1-m4 muscarinic acetylcholine receptor immunoreactivity in septohippocampal neurons and other identified hippocampal afferents

The Journal of Comparative Neurology, 1996
Muscarinic cholinergic transmission plays an important role in modulating hippocampal activity and many higher brain functions. Many of the modulatory effects of acetylcholine on hippocampal function result from direct effects in the hippocampus or from actions on the hippocampal afferent neurons.
S T, Rouse, A I, Levey
openaire   +2 more sources

Effects of Muscarinic Acetylcholine m1 and m4 Receptor Blockade on Dyskinesia in the Hemi-Parkinsonian Rat

Neuroscience, 2019
Standard treatment for Parkinson's disease (PD) is L-DOPA, but with chronic administration the majority of patients develop L-DOPA-induced dyskinesia (LID). Emerging evidence implicates the cholinergic system in PD and LID. Muscarinic acetylcholine receptors (mAChR) are known to modulate movement and of late have been implicated as possible targets for
Nicole E, Chambers, Samantha M, Meadows, Anne, Taylor, Eitan, Sheena, Kathryn, Lanza, Melissa M, Conti, Christopher, Bishop   +6 more
openaire   +2 more sources