Dualsteric Agonist for M2 Muscarinic Receptor Causes Oxidative Stress and Mitochondrial Alteration in Human Glioblastoma Cancer Stem Cells. [PDF]
Dualsteric agonist N8‐iper shows cytotoxic effects on glioblastoma cancer stem cells, but not on human normal astrocytes. Lipid accumulation appears as a consequence of cytotoxic stress; in fact, they are not present in healthy astrocytes. ABSTRACT Glioblastoma (GB) is the most malignant form of human brain tumor, characterized by heterogeneous cell ...
Guerriero C +11 more
europepmc +2 more sources
The dual-site agonist for human M2 muscarinic receptors Iper-8-naphtalimide induces mitochondrial dysfunction in Saccharomyces cerevisiae [PDF]
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
Synergistic mechanisms of medullary cholinergic-serotonergic pathway interactions in regulating neuronal excitability and locomotor activities [PDF]
Medullary serotonergic (5-HT) neurons play a pivotal role in locomotor initiation. While these neurons receive cholinergic innervation, the functional consequences and underlying mechanisms remain poorly understood. Using ePet-EYFP transgenic mice (P3–P6)
Yi Cheng +3 more
doaj +2 more sources
Gomisin E attenuates pentobarbital-induced sleep deficits in aging-related insomnia: an in vivo and in silico study implicating cholinergic signaling [PDF]
ObjectiveTo investigate the therapeutic effects of gomisin E on insomnia in aged rats and to elucidate the underlying mechanisms.MethodsAn aging-related insomnia rat model was established by intraperitoneal injection of D-galactose combined with p ...
Fan Yang +3 more
doaj +2 more sources
Muscarinic receptor regulation of chronic pain-induced atrial fibrillation
Atrial fibrillation (AF), one of the most common arrhythmias, is associated with chronic emotional disorder. Chronic pain represents a psychological instability condition related to cardiovascular diseases, but the mechanistic linkage connecting chronic ...
Chao Gong +10 more
doaj +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
General anesthesia produces multiple side effects. Notably, it temporarily impairs gastrointestinal motility following surgery and causes the so-called postoperative ileus (POI), a multifactorial and complex condition that develops secondary to ...
Alexander V. Zholos +3 more
doaj +1 more source
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
.: Intestinal myofibroblasts (IMFs) that exist adjacent to the basement membrane of intestines have contractility and contribute to physical barriers of the intestine.
Koichi Iwanaga +4 more
doaj +1 more source
Dysfunctional Presynaptic M2 Receptors in the Presence of Chronically High Acetylcholine Levels: Data from the PRiMA Knockout Mouse. [PDF]
The muscarinic M2 receptor (M2R) acts as a negative feedback regulator in central cholinergic systems. Activation of the M2 receptor limits acetylcholine (ACh) release, especially when ACh levels are increased because acetylcholinesterase (AChE) activity
Franziska Mohr +3 more
doaj +1 more source

