Structural determinants at the M2 muscarinic receptor modulate the RGS4-GIRK response to pilocarpine by impairment of the receptor voltage sensitivity [PDF]
Membrane potential controls the response of the M2 muscarinic receptor to its ligands. Membrane hyperpolarization increases response to the full agonist acetylcholine (ACh) while decreasing response to the partial agonist pilocarpine.
I-Shan Chen+2 more
doaj +2 more sources
Non-Neuronal Functions of the M2 Muscarinic Acetylcholine Receptor [PDF]
Acetylcholine is an important neurotransmitter whose effects are mediated by two classes of receptors. The nicotinic acetylcholine receptors are ion channels, whereas the muscarinic receptors belong to the large family of G protein coupled seven ...
Wymke Ockenga+4 more
semanticscholar +5 more sources
The role of muscarinic receptors in the beneficial effects of adenosine against myocardial reperfusion injury in rats. [PDF]
Adenosine, a catabolite of ATP, displays a wide variety of effects in the heart including regulation of cardiac response to myocardial ischemia and reperfusion injury.
Lei Sun+8 more
doaj +1 more source
First-in-Human Assessment of 11C-LSN3172176, an M1 Muscarinic Acetylcholine Receptor PET Radiotracer
Visual Abstract This was a first-in-human study of the PET radiotracer 11C-LSN3172176 for the muscarinic acetylcholine receptor subtype M1. The objectives of the study were to determine the appropriate kinetic model to quantify binding of the tracer to ...
M. Naganawa+15 more
semanticscholar +1 more source
Evolution of the Muscarinic Acetylcholine Receptors in Vertebrates [PDF]
The family of muscarinic acetylcholine receptors (mAChRs) consists of five members in mammals, encoded by the CHRM1-5 genes. The mAChRs are G-protein-coupled receptors, which can be divided into the following two subfamilies: M2 and M4 receptors coupling to Gi/o; and M1, M3, and M5 receptors coupling to Gq/11.
Julia E. Pedersen+2 more
openaire +4 more sources
M1 muscarinic acetylcholine receptor dysfunction in moderate Alzheimer’s disease pathology
Aggregation of amyloid beta and loss of cholinergic innervation in the brain are predominant components of Alzheimer’s disease pathology and likely underlie cognitive impairment.
J. Yi+6 more
semanticscholar +1 more source
Allosteric Modulation of Muscarinic Acetylcholine Receptors [PDF]
Muscarinic acetylcholine receptors (mAChRs) are prototypical Family A G protein coupled-receptors. The five mAChR subtypes are widespread throughout the periphery and the central nervous system and, accordingly, are widely involved in a variety of both physiological and pathophysiological processes.
Arthur Christopoulos+2 more
openaire +3 more sources
Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers [PDF]
Each subtype of the muscarinic receptor family of G protein-coupled receptors is activated by similar concentrations of the neurotransmitter acetylcholine or closely related synthetic analogs such as carbachol. However, pharmacological selectivity can be
Alvarez-Curto, Elisa+3 more
core +1 more source
Involvement of muscarinic receptors in psychomotor hyperactivity in dopamine-deficient mice
Dopamine-deficient (DD) mice exhibit psychomotor hyperactivity that might be related to a decrease in muscarinic signaling. In the present study, muscarinic acetylcholine receptor M2 (CHRM2) density decreased in the cortex in DD mice. This is significant
Masayo Fujita+6 more
doaj +1 more source
An in vivo biosensor for neurotransmitter release and in situ receptor activity. [PDF]
Tools from molecular biology, combined with in vivo optical imaging techniques, provide new mechanisms for noninvasively observing brain processes. Current approaches primarily probe cell-based variables, such as cytosolic calcium or membrane potential ...
Griesbeck, Oliver+6 more
core +2 more sources