Monoamine Oxidase Inhibition by Major Tanshinones From Salvia Miltiorrhiza and Selective Muscarinic Acetylcholine M4 Receptor Antagonism by Tanshinone I [PDF]
Biomolecules, 2021 Monoamine oxidases (MAOs) and muscarinic acetylcholine receptors (mAChRs) are considered important therapeutic targets for Parkinson’s disease (PD). Lipophilic tanshinones are major phytoconstituents in the dried roots of Salvia miltiorrhiza that have ...
Ritu Prajapati +6 more
semanticscholar +4 more sources
Discovery of VU6016235: A Highly Selective, Orally Bioavailable, and Structurally Distinct Tricyclic M4 Muscarinic Acetylcholine Receptor Positive Allosteric Modulator (PAM). [PDF]
ACS Chem NeurosciHerein, 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 ...
Engers JL +17 more
europepmc +2 more sources
Involvement of Cyclin Dependent Kinase 5 in M4 Muscarinic Acetylcholine Receptor-Mediated Cholinergic Transmission within the Mouse Dorsal Striatum [PDF]
, 2021 Background: An imbalance between dopamine (DA) and acetylcholine (ACh) within the striatum has reemerged as key to the pathophysiology of the neurodegenerative disorder, Parkinson's disease (PD). M4 is a prominent muscarinic ACh receptor subtype in the
Hu Zhou +9 more
openalex +2 more sources
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 +3 more
doaj +3 more sources
African-specific variability in the acetylcholine muscarinic receptor M4: association with cocaine and heroin addiction. [PDF]
Pharmacogenomics, 2016 AIM This study was designed to determine whether polymorphisms in acetylcholine receptors contribute to opioid dependence and/or cocaine dependence. PATIENTS & METHODS The sample (n = 1860) was divided by drug and ancestry, and 55 polymorphisms (nine ...
O. Levran +7 more
semanticscholar +5 more sources
Molecular Brain, 2016 BackgroundThe development of the nervous system involves an initially exuberant production of neurons that make an excessive number of synaptic contacts. The initial overproduction of synapses promotes connectivity. Hebbian competition between axons with
Laura Nadal +7 more
openalex +2 more sources
Detection and Quantification of Allosteric Modulation of Endogenous M4 Muscarinic Acetylcholine Receptor Using Impedance-Based Label-Free Technology in a Neuronal Cell Line [PDF]
Journal of biomolecular screening, 2014 Allosteric modulators of G protein–coupled receptors have the potential to achieve greater receptor subtype selectivity compared with ligands targeting the orthosteric site of this receptor family.
Amy N. Y. Chen +5 more
openalex +2 more sources
Antipsychotic-induced catalepsy is attenuated in mice lacking the M4 muscarinic acetylcholine receptor [PDF]
European Journal of Pharmacology, 2011 A delicate balance exists between the central dopaminergic and cholinergic neurotransmitter systems with respect to motor function. An imbalance can result in motor dysfunction as observed in Parkinson's disease patients and in patients treated with antipsychotic compounds.
Anders Fink‐Jensen +6 more
openalex +5 more sources
Acetylcholine regulates the melanogenesis of retinal pigment epithelia cells via a cAMP-dependent pathway: A non-neuronal function of cholinergic system in retina [PDF]
HeliyonThe turnover rate of melanogenesis in retinal pigment epithelium (RPE) and its molecular signaling remain unclear. This study aimed to investigate the role of cholinergic signaling in the process of melanogenesis of cultured RPE cells.
Ivan Kong +6 more
doaj +2 more sources