A5079831474- Neuroscience and Neuropharmacology Research
- Receptor Mechanisms and Signaling
- Chemical Synthesis and Analysis
- Nicotinic Acetylcholine Receptors Study
- Chemistry and Chemical Engineering
- Amino Acid Enzymes and Metabolism
- Pain Mechanisms and Treatments
- Pharmacological Receptor Mechanisms and Effects
- Alkaloids: synthesis and pharmacology
- Ion channel regulation and function
- Cholinesterase and Neurodegenerative Diseases
- Alzheimer's disease research and treatments
- Memory and Neural Mechanisms
- Neurotransmitter Receptor Influence on Behavior
- Computational Drug Discovery Methods
- Bioactive Compounds and Antitumor Agents
- Psychedelics and Drug Studies
Inserm
2022-2025
Centre National de la Recherche Scientifique
2022-2025
Université de Montpellier
2022-2025
Institut des Biomolécules Max Mousseron
2022-2024
Institut de Génomique Fonctionnelle
2022-2024
École Nationale Supérieure de Chimie de Montpellier
2022-2023
Abstract Synthetic mechanochemistry, the use of mechanical force produced by milling, grinding or extruding, as an activation technique, provides access to chemical entities all kinds. This Review is focused on examples reported so far known Active Pharmaceutical Ingredients (APIs), and effectively evaluated bioactive molecules, prepared mechanosynthesis. Three families molecules are discussed: heterocyclic compounds, metal complexes peptides. Advantages mechanochemistry approach highlighted...
Bambuterol is a long-acting anti-asthmatic prodrug which releases terbutaline. Terbutaline an agonist of the β2-adrenergic receptors formed by decarbamoylation bambuterol butyrylcholinesterase. Inhibition latter, as well activation β2-AR, are interest for treatment Alzheimer's disease (AD). Combining these two activities, could express good clinical efficacy against AD. The present work firstly confirmed capacity to display in cellulo neuroprotective reduction Tau hyperphosphorylation and...
The multifactorial origin and neurochemistry of Alzheimer's disease (AD) call for the development multitarget treatment strategies. We report a first-in-class triple acting compound that targets serotonin type 6 3 receptors (5-HT-Rs) monoamine oxidase B (MAO-B) as an approach treating AD. key structural features required MAO-B inhibition 5-HT6R antagonism interaction with 5-HT3R were determined using molecular dynamic simulations cryo-electron microscopy, respectively. Bioavailable PZ-1922...
ou non, émanant des établissements d'enseignement et de recherche français étrangers, laboratoires publics privés.
The serotonin type 6 receptor (5-HT6R) displays a strong constitutive activity, suggesting it participates largely in the physiological and pathological processes controlled by receptor. active states of 5-HT6R engage particular signal transduction pathways that lead to different biological responses. In this study, we present development neutral antagonists at Gs signaling built upon 2-phenylpyrrole scaffold. Using molecular dynamics simulations, outline relationship between exposure basic...
In addition to the canonical Gs adenylyl cyclase pathway, serotonin type 6 receptor (5-HT6R) recruits additional signaling pathways that control cognitive function, brain development, and synaptic plasticity in an agonist-dependent independent manner. Considering aberrant constitutive agonist-induced active states are involved various pathological mechanisms, development of biased ligands with different functional profiles at specific 5-HT6R-elicited may provide a novel therapeutic...
The serotonin type 6 receptor (5-HT6R) displays a strong constitutive activity, suggesting it participates largely in the physiological and pathological processes controlled by receptor. active states of 5-HT6R engage particular signal transduction pathways that lead to different biological responses. In this study, we present development neutral antagonists at Gs signaling built upon 2-phenylpyrrole scaffold. Using molecular dynamics simulations, outline relationship between exposure basic...
Salt bridge (SB, double-charge-assisted hydrogen bonds) formation is one of the strongest molecular non-covalent interactions in biological systems, including ligand–receptor complexes. In case G-protein-coupled receptors, such an interaction formed by conserved aspartic acid (D3.32) residue and basic moiety aminergic ligand. This study aims to determine influence substitution pattern at nitrogen atom geometry amine position 4 1H-pyrrolo[3,2-c]quinoline on quality salt 5-HT6 receptor D3...