Search results for "acetylcholine."

Acetylcholine receptors (muscarinic) in GtoPdb v.2021.3

2021

Muscarinic acetylcholine receptors (mAChRs) (nomenclature as agreed by the NC-IUPHAR Subcommittee on Muscarinic Acetylcholine Receptors [50]) are activated by the endogenous agonist acetylcholine. All five (M1-M5) mAChRs are ubiquitously expressed in the human body and are therefore attractive targets for many disorders. Functionally, M1, M3, and M5 mAChRs preferentially couple to Gq/11 proteins, whilst M2 and M4 mAChRs predominantly couple to Gi/o proteins. Both agonists and antagonists of mAChRs are clinically approved drugs, including pilocarpine for the treatment of elevated intra-ocular pressure and glaucoma, and atropine for the treatment of bradycardia and poisoning by muscarinic age…

Persistent activity in layer 5 pyramidal neurons following cholinergic activation of mouse primary cortices

2011

Persistent spiking activity is thought to be a cellular process involved in working memory. We have been interested in whether persistent activity also exists in cortical areas which are not involved in this memory process. To study the possible presence and the mechanisms of persistent activity in layer 5 pyramidal cells of the mouse primary somatosensory, visual and motor cortices, we used patch-clamp and calcium imaging techniques. A combination of cholinergic receptor activation and suprathreshold depolarization or sufficient extracellular stimulation leads to either a subthreshold afterdepolarization or suprathreshold persistent activity in these cortices. There is a continuum of respo…

Contraction of human airways by oxidative stress

1999

We examined the in vitro effects of tert-butylhydroperoxide (tBu-OOH) in human bronchial muscle. tert-Butylhydroperoxide produced concentration-dependent contractions of bronchial rings (maximum effect was 56.5 +/- 9.6% of contraction by 1 mM acetylcholine; effective concentration 50% was approximately 100 microM). tert-Butylhydroperoxide (0.5 mM)-induced contraction was enhanced by epithelial removal but abolished by indomethacin (cyclooxygenase inhibitor) and zileuton (lipoxygenase inhibitor). tert-Butylhydroperoxide produced a transient rise in intracellular calcium in human cultured airway smooth muscle cells (HCASMC). The bronchial reactivity to acetylcholine and histamine was not alte…

Response and Recovery of Brain Acetylcholinesterase Activity in the European Eel,Anguilla anguilla,Exposed to Fenitrothion

1998

European eel (Anguilla anguilla) were exposed to sublethal fenitrothion concentrations in a continuous flow-through system for 4 days. Brain acetylcholinesterase (AChE) activity was evaluated after 2, 8, 12, 24, 32, 48, 56, 72, and 96 h pesticide exposure. Results indicated that AChE activity in eel brains decreased as the concentration of fenitrothion increased. The pesticide induced significant inhibitory effects on the AChE activity ofA. anguilla,ranging from >40% inhibition at a sublethal concentration of 0.02 ppm to >60% inhibition at a sublethal concentration of 0.04 ppm. Eel were exposed to both fenitrothion concentrations for 96 h and then allowed a period of recovery in pesticide-f…

Central nicotinic receptors, neurotrophic factors and neuroprotection

2000

The multiple combinations of nAChR subunits identified in central nervous structures possess distinct pharmacological and physiological properties. A growing number of data have shown that compounds interacting with neuronal nAChRs have, both in vivo and in vitro, the potential to be neuroprotective and that treatment with nAChR agonists elicit long-lasting improving of cognitive performance in a variety of behavioural tests in rats, monkeys and humans. Epidemiological and clinical studies suggested also a potential neuroprotective/trophic role of (-)-nicotine in neurodegenerative disease, such as Alzheimer's and Parkinson's disease. Taken together experimental and clinical data largely ind…

Hsp60 is actively secreted by human tumor cells

2010

Background Hsp60, a Group I mitochondrial chaperonin, is classically considered an intracellular chaperone with residence in the mitochondria; nonetheless, in the last few years it has been found extracellularly as well as in the cell membrane. Important questions remain pertaining to extracellular Hsp60 such as how generalized is its occurrence outside cells, what are its extracellular functions and the translocation mechanisms that transport the chaperone outside of the cell. These questions are particularly relevant for cancer biology since it is believed that extracellular chaperones, like Hsp70, may play an active role in tumor growth and dissemination. Methodology/Principal Findings S…

Enzyme-Controlled Nanodevice for Acetylcholine-Triggered Cargo Delivery Based on Janus Au–Mesoporous Silica Nanoparticles

2017

[EN] This work reports a new gated nanodevice for acetylcholine-triggered cargo delivery. We prepared and characterized Janus Au-mesoporous silica nanoparticles functionalized with acetylcholinesterase on the Au face and with supramolecular b-cyclodextrin: benzimidazole inclusion complexes as caps on the mesoporous silica face. The nanodevice is able to selectively deliver the cargo in the presence of acetylcholine via enzyme-mediated acetylcholine hydrolysis, locally lowering the pH and opening the supramolecular gate. Given the key role played by ACh and its relation with Parkinson's disease and other nervous system diseases, we believe that these findings could help design new therapeuti…

Nicotinic Receptors in Human Brain

1994

A vast knowledge is currently available on the molecular biology and the pharmacology of nicotinic acetylcholine receptors (nAChR) in the mammalian central nervous system (CNS) (Sargent, 1993). Only few attempts have been made to approach the expression of nAChRs at the level of functional systems, considering the different cell types involved and their connectivity. This aspect is of particular importance in order to evaluate nAChR expression under pathological conditions. Histochemical techniques have proven to be useful since immunohistochemistry and in situ hybridization can be performed on human autopsy tissue and allow for a cell type-specific localization of nAChR proteins and nAChR …

Expression of muscarinic receptors on the murine embryonic stem cell line CGR8

2013

Murine muscle engineered from dermal precursors: an in vitro model for skeletal muscle generation, degeneration and fatty infiltration.

2013

Skeletal muscle can be engineered by converting dermal precursors into muscle progenitors and differentiated myocytes. However, the efficiency of muscle development remains relatively low and it is currently unclear if this is due to poor characterization of the myogenic precursors, the protocols used for cell differentiation, or a combination of both. In this study, we characterized myogenic precursors present in murine dermospheres, and evaluated mature myotubes grown in a novel three-dimensional culture system. After 5-7 days of differentiation, we observed isolated, twitching myotubes followed by spontaneous contractions of the entire tissue-engineered muscle construct on an extracellul…