Identification and Role of Muscarinic Receptor Subtypes Expressed in Rat Adrenal Medullary Cells
.: The muscarinic receptor is known to be involved in the acetylcholine (ACh)-induced secretion of catecholamines in the adrenal medullary (AM) cells of various mammals.
Keita Harada +4 more
doaj +1 more source
Effects of novel muscarinic M3 receptor ligand C1213 in pulmonary arterial hypertension models. [PDF]
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
core +2 more sources
Light-Activated Pharmacological Tools for Exploring the Cholinergic System. [PDF]
ABSTRACT Cholinergic transmission plays a critical role in both the central and peripheral nervous systems, affecting processes such as learning, memory, and inflammation. Conventional cholinergic drugs generally suffer from poor selectivity and temporal precision, leading to undesired effects and limited therapeutic efficacy. Photopharmacology aims to
Colleoni A +5 more
europepmc +2 more sources
Virtual Affinity Fingerprints for Target Fishing: A New Application of Drug Profile Matching [PDF]
We recently introduced Drug Profile Matching (DPM), a novel virtual affinity fingerprinting bioactivity prediction method. DPM is based on the docking profiles of ca.
Czobor, P. +6 more
core +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
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
Synergistic Antiemetic Effects of Nerolidol on Domperidone, Hyoscine, and Ondansetron: In Vivo and in Silico Investigations on Receptor Binding Affinity. [PDF]
Nerolidol shows prominent antiemetic activity and mitigates CuSO4.H2O‐mediated retching in chicks efficiently through its peripheral action. Additionally, the in silico studies have also shown possible antiemetic effects with greater binding affinity against muscarinic (specially, M2 and M3) and dopaminergic receptors.
Ghosh Situ S +7 more
europepmc +2 more sources
Identification of a Novel Allosteric Site at the M5Muscarinic Acetylcholine Receptor
The M5 muscarinic acetylcholine receptor (mAChR) has emerged as an exciting therapeutic target for the treatment of addiction and behavioral disorders. This has been in part due to promising preclinical studies with the M5 mAChR selective negative allosteric modulator (NAM), ML375. The binding site of ML375 remains unknown, however, making it difficult
Wessel A. C. Burger +13 more
openaire +2 more sources
Mir-34a-5p Mediates Cross-Talk between M2 Muscarinic Receptors and Notch-1/EGFR Pathways in U87MG Glioblastoma Cells: Implication in Cell Proliferation [PDF]
Glioblastoma (GBM) is the most aggressive human brain tumor. The high growth potential and decreased susceptibility to apoptosis of the glioma cells is mainly dependent on genetic amplifications or mutations of oncogenic or pro-apoptotic genes ...
Bevilacqua, Valeria +8 more
core +2 more sources
Assessment of the molecular mechanisms of action of novel 4-phenylpyridine-2-one and 6-phenylpyrimidin-4-one allosteric modulators at the M1 muscarinic acetylcholine receptors [PDF]
Positive allosteric modulators (PAMs) that target the M1 muscarinic acetylcholine (ACh) receptor (M1 mAChR) are potential treatments for cognitive deficits in conditions such as Alzheimer's disease and schizophrenia.
Andrew B. Tobin +15 more
core +2 more sources

