Signaling Bias and Antagonism of Pilocarpine for M3 Muscarinic Acetylcholine Receptor
Pilocarpine is a prototypical drug used to treat glaucoma and dry mouth since the 19 th century and classified as either a full or partial muscarinic agonist. Here, we report several unexpected results pertaining to its interaction with its main therapeutic target ‐ muscarinic M3 receptor ...
Alexey N. Pronin +2 more
openaire +1 more source
Recent studies have reported the role of the M3 muscarinic acetylcholine receptor (M3R), a member of the G‐protein coupled receptor superfamily, encoded by the CHRM3 gene, in cardiac function and the regulation of blood pressure (BP).
Xi Zhang +22 more
doaj +1 more source
Parasympathetic activation in the anterior eye segment regulates various physiological functions. This process, mediated by muscarinic acetylcholine receptors, also impacts intraocular pressure (IOP) through the trabecular meshwork. While FDA-approved M3
Minjae J. Kim +4 more
doaj +1 more source
Effect of Eugenol on Detrusor Muscle: Potential for Overactive Bladder Treatment [PDF]
Purpose This investigation was conducted to elucidate the effects of eugenol on bladder contractility through experimental and in silico approaches. Methods To assess the impact of eugenol on muscular contractility, longitudinal strips of bladder tissue,
Marília Cavalcante Araújo +8 more
doaj +1 more source
A fast genetically encoded fluorescent sensor for faithful in vivo acetylcholine detection in mice, fish, worms and flies [PDF]
Here we design and optimize a genetically encoded fluorescent indicator, iAChSnFR, for the ubiquitous neurotransmitter acetylcholine, based on a bacterial periplasmic binding protein.
Borden, Philip M. +4 more
core
Denervation suppresses gastric tumorigenesis [PDF]
The nervous system plays an important role in the regulation of epithelial homeostasis and has also been postulated to play a role in tumorigenesis. We provide evidence that proper innervation is critical at all stages of gastric tumorigenesis.
Andersen, Goran T. +20 more
core +1 more source
Macrophage TNF-α mediates parathion-induced airway hyperreactivity in guinea pigs. [PDF]
Organophosphorus pesticides (OPs) are implicated in human asthma. We previously demonstrated that, at concentrations that do not inhibit acetylcholinesterase activity, the OP parathion causes airway hyperreactivity in guinea pigs as a result of ...
Allison D. Fryer +12 more
core +1 more source
Teaching an Old Drug New Tricks: Agonism, Antagonism, and Biased Signaling of Pilocarpine through M3 Muscarinic Acetylcholine Receptor [PDF]
Alexey Pronin +2 more
openalex +1 more source
Effects of Nerve Growth Factor shRNA Inhibition on Asthma Phenotypes in a Mouse Model of Asthma
Nerve growth factor (NGF) plays an important role in airway hyper-responsiveness (AHR). In this study, we aimed at investigating the effect of NGF inhibition on AHR and other asthma phenotypes in a mouse model of asthma.
Jinhong Wu +3 more
doaj
G fehérjék szerepe a húgyhólyag simaizom-működésének szabályozásában. = G protein-mediated regulation of urinary smooth muscle contractility. [PDF]
Eredményeink szerint élettani körülmények között a Gq/11 jelátviteli út (vélhetőleg az M3-receptorok által aktiválva) döntő szerepet játszik az acetilkolin simaizom-kontrakciót okozó hatásának közvetítésében és ezáltal a húgyhólyag működésének ...
Benyó, Zoltán
core

