Analogs of compound 1 with a variety of azacycles and heteroaryl groups were synthesized. These analogs exhibited Ki values ranging from 0.15 to > 10,000 nM when tested in vitro for cholinergic channel receptor binding activity (displacement of [3H](-) cytisine from whole rat brain synaptic membranes).
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(99)00462-x | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
MuSK regulates neuromuscular junction Nav1.4 localization and excitability.
J Neurosci
January 2025
Carney Institute for Brain Science, Brown University, Providence, RI 02912
The neuromuscular junction (NMJ) is the linchpin of nerve-evoked muscle contraction. Broadly, the function of the NMJ is to transduce nerve action potentials into muscle fiber action potentials (MFAPs). Efficient neuromuscular transmission requires both cholinergic signaling, responsible for generation of endplate potentials (EPPs), and excitation, the amplification of the EPP by postsynaptic voltage-gated sodium channels (Nav1.
View Article and Find Full Text PDFNovel multipotent conjugate bearing tacrine and donepezil motifs with dual cholinergic inhibition and neuroprotective properties targeting Alzheimer's disease.
RSC Med Chem
January 2025
Área de Neurofisiología celular, Instituto de Biología, Facultad de Ciencias Exactas y Naturales, Universidad de Antioquia Medellín Colombia
In this work, we developed potential multifunctional agents to combat Alzheimer's disease. According to our strategy, fragments of tacrine and donepezil were merged in a unique hybrid structure. After successfully synthesizing the compounds, they were evaluated for their dual AChE/BuChE inhibitor potential and neuroprotector response using a glutamate-induced excitotoxicity model.
View Article and Find Full Text PDFCHOLINERGIC MODULATION OF CELLULAR RESONANCE IN NON-HUMAN PRIMATE HIPPOCAMPUS.
bioRxiv
January 2025
Department of Neurobiology and Biophysics, University of Washington School of Medicine, Seattle, WA 98195-7290, USA.
Acetylcholine modulates the network physiology of the hippocampus, a crucial brain structure that supports cognition and memory formation in mammals . In this and adjacent regions, synchronized neuronal activity within theta-band oscillations (4-10Hz) is correlated with attentive processing that leads to successful memory encoding . Acetylcholine facilitates the hippocampus entering a theta oscillatory regime and modulates the temporal organization of activity within theta oscillations .
View Article and Find Full Text PDFCharacterization of cell membrane fragments containing muscle type nAChR from Tetronarce californica after preparation using high pressure homogenization.
Toxicol Lett
January 2025
Bundeswehr Institute for Pharmacology and Toxicology, Neuherbergstraße 11, Munich 80937, Germany. Electronic address:
The nicotinic acetylcholine receptor (nAChR) is a pentameric ligand-gated ion channel (pLGIC) commonly used as a model for receptors belonging to the Cys-loop superfamily. Members of pLGICs are standardly used in numerous toxicological investigations e.g.
View Article and Find Full Text PDFEfficacy and safety of botulinum toxin injection in the management of chronic symptomatic anal fissure: a systematic review and meta-analysis of randomized controlled trials.
Tech Coloproctol
January 2025
Royal Glamorgan Hospital, Llantrisant, Wales, UK.
Background: Anal fissure is one of the most painful anal conditions. Various management options are available, including topical nitrites, calcium channel blockers, botulinum toxin injection, and lateral internal sphincterotomy. This study aimed to assess the efficacy and safety of botulinum toxin A (BT) injection for the management of symptomatic chronic anal fissures by conducting a systematic review of the literature and meta-analysis of published randomized controlled trials (RCTs).
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!