Results 31 to 40 of about 13,541 (253)
G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular effector proteins. Different agonists can promote differential receptor-induced signaling responses – termed bias – potentially by eliciting ...
Anja Flöser +6 more
doaj +1 more source
Structure-guided development of selective M3 muscarinic acetylcholine receptor antagonists [PDF]
Significance The development of selective antagonists for muscarinic acetylcholine receptors is challenging due to high homology in orthosteric binding sites among subtypes. Starting from a single amino acid difference in the orthosteric pockets in M2 muscarinic acetylcholine receptor (M2R) and M3R, we developed an M3R-selective antagonist ...
Liu, Hongtao +19 more
openaire +4 more sources
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
M3 muscarinic acetylcholine receptor–reactive Th17 cells in primary Sjögren’s syndrome [PDF]
M3 muscarinic acetylcholine receptor (M3R) is one of the autoantigens associated with Sjögren's syndrome (SS) and is localized in exocrine glands where disease-specific inflammation occurs. The inflammatory lesion is characterized by infiltration of CD4+ T cells, including clonally expanded Th17 cells.
Saori Abe +11 more
openaire +2 more sources
Is there a rationale and role for long-acting anticholinergic bronchodilators in asthma? [PDF]
The authors acknowledge the medical writing assistance received from Sam Yarwood, PhD, of Complete HealthVizion, in the form of literature searches and preparation and revision of the draft manuscript.Peer reviewedPublisher ...
Fromer, Leonard +4 more
core +7 more sources
.: 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
We investigated pharmacological characteristics of the itch-associated response to chronic dermatitis induced by 4-ethoxymethylene-2-phenyl-2-oxazolin-5-one (oxazolone) repeated application in mice.
Yukihito Tsukumo +2 more
doaj +1 more source
Irritable bowel syndrome (IBS) is a chronic functional bowel disorder characterized by intestinal dysmotility. Changes in intestinal microbiota (dysbiosis) can lead to alterations in neuro-muscular functions in the gut. Toll-like receptors (TLRs) 2 and 4
Elena Layunta +2 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
Expression of muscarinic acetylcholine receptors M3 and M5 in osteoporosis [PDF]
Cholinergic signaling via muscarinic acetylcholine receptors (mAChR) is known to influence various physiological functions. In bone, M3 mAChR and M5 mAChR were identified on the membrane of osteoblast-like cells. M3 mAChR seems to be particularly relevant for bone physiology, as signaling via this receptor was reported to increase bone formation and ...
Kauschke, Vivien +3 more
openaire +2 more sources

