1. The effects of a high molecular weight toxin isolated from the sea anemone Condylactis gigantea (Condytoxina 2) on the cholinergic responses were studied in two different preparations: identified cells of a land snail and enzymatically dissociated mice sensory neurons. These neurons were studied using intracellular recording and concentration clamp techniques respectively. 2. The toxin produces a concentration-dependent dual effect on the cholinergic responses in both preparations. Thus the application of the toxin at concentrations up to 25 nmol/l produces a reversible block of the response whereas higher doses potentiates it. 3. These results suggest that Condytoxina 2 contains an active compound(s) with the capacity to bind to the nicotinic acetylcholine receptor of excitable cells in both snail and mice neurons. During this action complex allosteric interactions among the binding sites could occur.
Download full-text PDF |
Source |
---|---|
http://dx.doi.org/10.1016/0742-8413(92)90029-7 | DOI Listing |
Neurochem Res
January 2025
Department of Biochemistry and Molecular Biology, Federal University of Santa Maria (UFSM), Santa Maria, RS, Brazil.
Purinergic signaling plays a major role in aging and neurodegenerative diseases, which are associated with memory decline. Blackcurrant (BC), an anthocyanin-rich berry, is renowned for its antioxidant and neuroprotective activities. However, evidence on the effects of BC on purinergic signaling is lacking.
View Article and Find Full Text PDFNeurotoxicology
January 2025
Laboratoire Physiologie, Ecologie and Environnement (P2E), Université d'Orléans, UR 1207, USC-INRAE 1328, 1 rue de Chartres, 45067 Orléans, France; Institut Universitaire de France (IUF), 1 rue Descartes 75005 Paris, France. Electronic address:
Although neonicotinoids were considered safe for mammals for many decades, recent research has proven that these insecticides can alter cholinergic functions by interacting with neuronal nicotinic acetylcholine (ACh) receptors (nAChRs). One such receptor is the heteromeric α4β2 nAChR, which exists under two different stoichiometries: high sensitivity and low sensitivity α4β2 nAChRs. To replace these insecticides, new classes of insecticides have been developed, such as, sulfoximine, sulfoxaflor, and the butanolide, flupyradifurone.
View Article and Find Full Text PDFChemistryOpen
January 2025
Department of Chemistry, Faculty of Sciences, University of Guilan, Rasht, 4193833697, Iran.
The inhibition of acetylcholinesterase (AChE), an enzyme responsible for the inactivation and decrease in acetylcholine in the cholinergic pathway, has been considered an attractive target for small-molecule drug discovery in Alzheimer's disease (AD) therapy. In the present study, a series of TZD derivatives were designed, synthesized, and studied for drug likeness, blood-brain barrier (BBB) permeability, and adsorption, distribution, metabolism, excretion, and toxicity (ADMET). Additionally, docking studies of the designed compounds were performed on AChE.
View Article and Find Full Text PDFPhytomedicine
December 2024
Department of Psychiatry and Psychotherapy, University Medical Center Mainz, Johannes Gutenberg-University Mainz, Mainz, Germany; Research Center for Immunotherapy (FZI), University Medical Center at the Johannes Gutenberg University Mainz, Mainz, Germany. Electronic address:
Background: Ginkgo biloba leaf extract EGb 761® has shown clinical efficacy in patients with mild cognitive impairment and dementia. However, the pharmacological action of EGb 761® in Alzheimer's disease (AD) remains unclear and molecular mechanisms targeted in the brain are not completely understood.
Hypothesis/purpose: We aimed to investigate 1) the potential sex-dependent effects of oral administration of EGb 761® in 5xFAD mice, an AD mouse model, and 2) the underlying microglial subtype responsible for the observed anti-inflammatory effects in the brain.
Am J Physiol Lung Cell Mol Physiol
January 2025
Smooth Muscle Research Centre, Dundalk Institute of Technology, Dublin Road, Dundalk, Co. Louth, Ireland.
Cholinergic tone is elevated in obstructive lung conditions such as COPD and asthma, but the cellular mechanisms underlying cholinergic contractions of airway smooth muscle (ASM) are still unclear. Some studies report an important role for L-type Ca channels (LTCC) and Ano1 Ca-activated Cl™ channels (CACC) in these responses, but others dispute their importance. Cholinergic contractions of ASM involve activation of M3Rs, however stimulation of M2Rs exerts a profound hypersensitisation of these responses.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!