Results 11 to 20 of about 46,071 (240)

Multitargeting nature of muscarinic orthosteric agonists and antagonists

Frontiers in Physiology, 2022
Muscarinic receptors (mAChRs) are typical members of the G protein-coupled receptor (GPCR) family and exist in five subtypes from M1 to M5. Muscarinic receptor subtypes do not sufficiently differ in affinity to orthosteric antagonists or agonists ...
Jaromir Myslivecek
doaj   +1 more source

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., Broad, Lisa M., Brooke, Simon M., Bundgaard, Christoffer, Christopoulos, Arthur, Crabtree, Michael D., Dwomoh, Louis, Felder, Christian C., Langmead, Christopher J., Mogg, Adrian J., Molloy, Colin, Sanger, Helen E., Sexton, Patrick M., Thompson, Karen J., Tobin, Andrew B.   +14 more
core   +1 more source

Cholinergic suppression: A postsynaptic mechanism of long-term associative learning [PDF]

, 1986
Food avoidance learning in the mollusc Pleurobranchaea entails reduction in the responsiveness of key brain interneurons in the feeding neural circuitry, the paracerebral feeding command interneurons (PCNs), to the neurotransmitter acetylcholine (AcCho).
Davis, W. Jackson, Kovac, Mark P., Matera, Eugene M., McCormack, Kenneth J., Morielli, Anthony D., Shrum, Richard G.   +5 more
core   +2 more sources

A Distinct Role of the Autonomic Nervous System in Modulating the Function of Lymphatic Vessels under Physiological and Tumor-Draining Conditions

Cell Reports, 2019
Summary: Lymphatic vessels (LVs) are important in the regulation of tissue fluid homeostasis and the pathogenesis of tumor progression. We investigated the innervation of LVs and the response to agonists and antagonists of the autonomic nervous system in 
Samia B. Bachmann, Denise Gsponer, Javier A. Montoya-Zegarra, Martin Schneider, Felix Scholkmann, Carlotta Tacconi, Simon F. Noerrelykke, Steven T. Proulx, Michael Detmar   +8 more
doaj   +1 more source

Exploring Adjunctive Novel Therapeutic Approach of KarXT (Xanomeline-Trospium Chloride) for Managing Psychotic Symptoms in Patients With Schizophrenia and Alzheimer's Disease. [PDF]

Brain Behav
An overview of the mechanism of action, clinical trials, and classical findings of KarXT for the management of psychotic symptoms in patients with schizophrenia and alzheimer's disease. ABSTRACT Background Acute psychotic symptoms like delusions and hallucinations are of major concern while treating patients with schizophrenia and alzheimer's psychosis,
Kanwal A, Azeem B, Nasir H, Mumtaz F, Ashraf N, Amin MHJ, Kanwal W, Khan BW.   +7 more
europepmc   +2 more sources

Cholinergic modulation of dopamine overflow in the rat neostriatum: A fast cyclic voltammetric study in vitro [PDF]

, 1994
Stimulus-evoked dopamine overflow in rat neostriatal slices was determined using fast cyclic voltammetry. The dopamine efflux induced by intrastriatal stimulation increased with stimulus intensity and was found to be enhanced by more than 100% upon ...
Kudernatsch, Martina, Sutor, Bernd
core   +1 more source

Muscarinic Receptor Agonists and Antagonists

Molecules, 2001
A comprehensive review of pharmacological and medical aspects of the muscarinic class of acetylcholine agonists and antagonists is presented. The therapeutic benefits of achieving receptor subtype selectivity are outlined and applications in the ...
David R. Kelly, Kenneth J. Broadley
doaj   +1 more source

Markers of muscarinic deficit for individualized treatment in schizophrenia

Frontiers in Psychiatry, 2023
Recent clinical studies have shown that agonists at muscarinic acetylcholine receptors effectively reduce schizophrenia symptoms. It is thus conceivable that, for the first time, a second substance class of procholinergic antipsychotics could become ...
Heiner Stuke, Heiner Stuke
doaj   +1 more source

A photoisomerizable muscarinic antagonist. Studies of binding and of conductance relaxations in frog heart [PDF]

, 1982
These experiments employ the photoisomerizable compound, 3,3'-bis- [alpha-(trimethylammonium)methyl]azobenzene (Bis-Q), to study the response to muscarinic agents in frog myocardium. In homogenates from the heart, trans-Bis-Q blocks the binding of [3H]-N-
Birdsall, Nigel J. M., Erlanger, Bernard F., Lester, Henry A., Nargeot, Joel, Stockton, Jane, Wassermann, Norbert H.   +5 more
core   +1 more source

Further Insights Into Anticholinergic Action Informed by Japanese Anticholinergic Risk Scale. [PDF]

Geriatr Gerontol Int
ABSTRACT The increased anticholinergic burden caused by medications in older adults is one of the adverse drug reactions of particular concern, as it can exacerbate the onset of geriatric syndromes or induce cognitive dysfunction, and is also related to the issue of polypharmacy.
Mogi M, Liu S, Suzuki Y, Shibata Y, Yamada S.   +4 more
europepmc   +2 more sources