Results 1 to 10 of about 24,220 (160)

Muscarinic Receptor Agonists and Antagonists [PDF]

open access: yesMolecules, 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   +2 more sources

The dual-site agonist for human M2 muscarinic receptors Iper-8-naphtalimide induces mitochondrial dysfunction in Saccharomyces cerevisiae [PDF]

open access: yesMicrobial Cell
Glioblastoma is a malignant astrocytic tumor of the brain. A significantly decrease of glioblastoma cell proliferation and survival can be achieved by activating the M2 muscarinic acetylcholine receptor (a G protein-coupled receptor, or GPCR) with two ...
Angela Cirigliano   +11 more
doaj   +2 more sources

Multitargeting nature of muscarinic orthosteric agonists and antagonists

open access: yesFrontiers 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   +3 more sources

Downstream Signaling of Muscarinic M4 Receptors Is Regulated by Receptor Density and Cellular Environment [PDF]

open access: yesPharmacology Research & Perspectives
Multiple muscarinic M4 receptor modulators are currently advancing in clinical development for the treatment of positive symptoms in schizophrenia, including agonists and positive allosteric modulators.
Madeleine Merz   +5 more
doaj   +2 more sources

Antipsychotic-like effect of the muscarinic acetylcholine receptor agonist BuTAC in non-human primates. [PDF]

open access: yesPLoS ONE, 2015
Cholinergic, muscarinic receptor agonists exhibit functional dopamine antagonism and muscarinic receptors have been suggested as possible future targets for the treatment of schizophrenia and drug abuse. The muscarinic ligand (5R,6R)-6-(3-butylthio-1,2,5-
Maibritt B Andersen   +6 more
doaj   +1 more source

The Bronchoprotective Effects of Dual Pharmacology, Muscarinic Receptor Antagonist and β2 Adrenergic Receptor Agonist Navafenterol in Human Small Airways

open access: yesCells, 2023
Bronchodilators and anti-inflammatory agents are the mainstream treatments in chronic obstructive and pulmonary disease (COPD) and asthma.
Joseph Antony Jude   +4 more
doaj   +1 more source

Oscillatory calcium release and sustained store-operated oscillatory calcium signaling prevents differentiation of human oligodendrocyte progenitor cells

open access: yesScientific Reports, 2022
Endogenous remyelination in demyelinating diseases such as multiple sclerosis is contingent upon the successful differentiation of oligodendrocyte progenitor cells (OPCs).
Richard A. Seidman   +4 more
doaj   +1 more source

Vibrational spectroscopy analysis of ligand efficacy in human M2 muscarinic acetylcholine receptor (M2R)

open access: yesCommunications Biology, 2021
Katayama et al. report a vibrational spectroscopic study using ATR–FTIR of the human M2 muscarinic acetylcholine receptor (M2R). Their work involves an extensive comparison of agonists, antagonists, and inverse agonists, in which they show that they C ...
Kota Katayama   +8 more
doaj   +1 more source

The metronomic combination of paclitaxel with cholinergic agonists inhibits triple negative breast tumor progression. Participation of M2 receptor subtype

open access: yesPLoS ONE, 2020
Triple negative tumors are more aggressive than other breast cancer subtypes and there is a lack of specific therapeutic targets on them. Since muscarinic receptors have been linked to tumor progression, we investigated the effect of metronomic therapy ...
Alejandro J. Español   +7 more
doaj   +2 more sources

Functional characterization of three G protein-coupled acetylcholine receptors in parasitic nematode Trichinella spiralis

open access: yesInternational Journal for Parasitology: Drugs and Drug Resistance, 2023
The physiological significance of metabotropic acetylcholine receptors in parasitic nematodes remains largely unexplored. Here, three different Trichinella spiralis G protein-coupled acetylcholine receptors (TsGAR-1, -2, and -3) were identified in the ...
Cáinà Nìng   +4 more
doaj   +1 more source

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