Structural determinants at the M2 muscarinic receptor modulate the RGS4-GIRK response to pilocarpine by impairment of the receptor voltage sensitivity [PDF]
Scientific Reports, 2017 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
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Distinct agonist regulation of muscarinic acetylcholine M2-M3 heteromers and their corresponding homomers [PDF]
, 2015 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
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Carbachol increases intracellular free calcium concentrations in human granulosa-lutein cells [PDF]
, 1992 We investigated whether the stimulation of human granulosa-lutein cells with muscarinic and nicotinic receptor agonists can cause increases in intracellular free calcium (Ca2+), using Fura-2 microfluorimetry.
Föhr, K. J. +3 more
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An in vivo biosensor for neurotransmitter release and in situ receptor activity. [PDF]
, 2010 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
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Bitopic binding mode of an M1 muscarinic acetylcholine receptor agonist associated with adverse clinical trial outcomes [PDF]
, 2018 The realisation of the therapeutic potential of targeting the M1 muscarinic acetylcholine receptor (M1 mAChR) for the treatment of cognitive decline in Alzheimer's disease has prompted the discovery of M1 mAChR ligands showing efficacy in alleviating ...
Bradley, Sophie J. +14 more
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Cholinergic Signaling, Neural Excitability, and Epilepsy
Molecules, 2021 Epilepsy is a common brain disorder characterized by recurrent epileptic seizures with neuronal hyperexcitability. Apart from the classical imbalance between excitatory glutamatergic transmission and inhibitory γ-aminobutyric acidergic transmission ...
Yu Wang, Bei Tan, Yi Wang, Zhong Chen
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The role of inhibitory G proteins and regulators of G protein signaling in the in vivo control of heart rate and predisposition to cardiac arrhythmias [PDF]
, 2012 Inhibitory heterotrimeric G proteins and the control of heart rate. The activation of cell signaling pathways involving inhibitory heterotrimeric G proteins acts to slow the heart rate via modulation of ion channels.
Ang, R, Opel, A, Tinker, A
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Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. [PDF]
, 2016 Pulmonary hypertension (PH) is a complex disease comprising a pathologic remodeling and thickening of the pulmonary vessels causing an after load on the right heart ventricle that can result in ventricular failure. Triggered by oxidative stress, episodes
Ahmed, Mohamed +5 more
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Ligand regulation of the quaternary organization of cell surface M3 muscarinic acetylcholine receptors analyzed by fluorescence resonance energy transfer (FRET) imaging and homogenous time-resolved FRET [PDF]
, 2010 Flp-In T-REx 293 cells expressing a wild type human M muscarinic acetylcholine receptor construct constitutively and able to express a Receptor Activated Solely by Synthetic Ligand (RASSL) form of this receptor on demand maintained response to the ...
Alvarez-Curto, Elisa +3 more
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Cholinergic control of visual categorisation in macaques
Frontiers in Behavioral Neuroscience, 2011 Acetylcholine (ACh) is a neurotransmitter acting via muscarinic and nicotinic receptors that is implicated in several cognitive functions and impairments, such as Alzheimer’s disease. It is believed to especially affect the acquisition of new information,
Nikolaos C. Aggelopoulos +5 more
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