A5089395805- Neuropeptides and Animal Physiology
- Pharmacological Receptor Mechanisms and Effects
- Receptor Mechanisms and Signaling
- Computational Drug Discovery Methods
- Cholinesterase and Neurodegenerative Diseases
- Nicotinic Acetylcholine Receptors Study
- Fullerene Chemistry and Applications
- Alzheimer's disease research and treatments
University of Würzburg
2019-2021
Abstract μ‐Opioid receptors (μ‐ORs) play a critical role in the modulation of pain and mediate effects most powerful analgesic drugs. Despite extensive efforts, it remains insufficiently understood how μ‐ORs produce specific living cells. We developed new fluorescent ligands based on μ‐OR antagonist E‐p ‐nitrocinnamoylamino‐dihydrocodeinone (CACO), that display high affinity, long residence time pronounced selectivity. Using these ligands, we achieved single‐molecule imaging surface cells at...
The enzyme butyrylcholinesterase (BChE) represents a promising target for imaging probes to potentially enable early diagnosis of neurodegenerative diseases like Alzheimer's disease (AD) and monitor progression in some forms cancer. In this study, we present the design, facile synthesis, vitro preliminary ex vivo evaluation morpholine-based, selective inhibitor human BChE as positron emission tomography (PET) tracer with pseudo-irreversible binding mode. We demonstrate novel protecting group strategy
Abstract μ‐Opioid receptors (μ‐ORs) play a critical role in the modulation of pain and mediate effects most powerful analgesic drugs. Despite extensive efforts, it remains insufficiently understood how μ‐ORs produce specific living cells. We developed new fluorescent ligands based on μ‐OR antagonist E‐p ‐nitrocinnamoylamino‐dihydrocodeinone (CACO), that display high affinity, long residence time pronounced selectivity. Using these ligands, we achieved single‐molecule imaging surface cells at...
Abstract Purpose A neuropathological hallmark of Alzheimer’s disease (AD) is the presence amyloid-β (Aβ) plaques in brain, which are observed a significant number cognitively normal, older adults as well. In AD, butyrylcholinesterase (BChE) becomes associated with β aggregates, making it promising target for imaging probes to support diagnosis AD. this study, we present synthesis, radiochemistry, vitro and preliminary ex vivo investigations selective, reversible BChE inhibitor PET-tracer...
Hochselektive fluoreszierende Liganden abgeleitet aus dem Schlafmohn, wurden von D. Calebiro, M. Decker et al. in ihrem Forschungsartikel auf S. 6014 entwickelt, um zu untersuchen, ob μ-Opioidrezeptoren (μ-ORs) Dimere der Plasmamembran bilden können. Die Verbindungen weisen eine lange Verweilzeit und hohe Affinität auf, kleine Fraktion kurzlebiger Homodimere konnte mithilfe dieser chemischen Werkzeuge durch Einzelmolekülmikroskopie nachgewiesen werden.