A5031340154- Radiopharmaceutical Chemistry and Applications
- Click Chemistry and Applications
- Medical Imaging Techniques and Applications
- Neurotransmitter Receptor Influence on Behavior
- Monoclonal and Polyclonal Antibodies Research
- Neuroscience and Neuropharmacology Research
- Chemical Synthesis and Analysis
- Receptor Mechanisms and Signaling
- Chemical Reactions and Isotopes
- Pharmacological Receptor Mechanisms and Effects
- Parkinson's Disease Mechanisms and Treatments
- Alzheimer's disease research and treatments
- Fluorine in Organic Chemistry
- Psychedelics and Drug Studies
- Advanced biosensing and bioanalysis techniques
- Nicotinic Acetylcholine Receptors Study
- Advanced Biosensing Techniques and Applications
- Peptidase Inhibition and Analysis
- Neurological disorders and treatments
- Synthesis and Biological Evaluation
- Nanoparticle-Based Drug Delivery
- Cyclopropane Reaction Mechanisms
- Drug Transport and Resistance Mechanisms
- Advanced MRI Techniques and Applications
- Chemical synthesis and alkaloids
University of Copenhagen
2016-2025
Rigshospitalet
2016-2025
Copenhagen University Hospital
2015-2025
TetraPlan
2024
Vita-Salute San Raffaele University
2019
Istituti di Ricovero e Cura a Carattere Scientifico
2019
Istituto di Ricovero e Cura a Carattere Scientifico San Raffaele
2019
University of Münster
2019
Johanniter-Krankenhaus Bonn
2019
Johannes Gutenberg University Mainz
2005-2011
We here describe a multimodality neuroimaging containing data from healthy volunteers and patients, acquired within the Lundbeck Foundation Center for Integrated Molecular Brain Imaging (Cimbi) in Copenhagen, Denmark. The is of particular relevance neurobiological research questions related to serotonergic transmitter system with its normative on subtype receptors 5-HT1A, 5-HT1B, 5-HT2A, 5-HT4 5-HT transporter (5-HTT), but can easily serve other purposes. Cimbi database biobank were formally...
The development of highly selective and fast biocompatible reactions for ligation cleavage has paved the way new diagnostic therapeutic applications pretargeted in vivo chemistry. concept bioorthogonal pretargeting attracted considerable interest, particular targeted delivery radionuclides drugs. In nuclear medicine, can provide increased target-to-background ratios at early time-points compared to traditional approaches. This reduces radiation burden healthy tissue and, depending on...
The application of prostate-specific membrane antigen (PSMA)–targeted α-therapy is a promising alternative to β<sup>−</sup>-particle–based treatments. <sup>211</sup>At among the potential α-emitters that are favorable for this concept. Herein, <sup>211</sup>At-based PSMA radiopharmaceuticals were designed, developed, and evaluated. <b>Methods:</b> To identify <sup>211</sup>At-labeled lead, surrogate strategy was applied. Because astatine does not exist as stable nuclide, it commonly replaced...
During the last decades polymer-based nanomedicine has turned out to be a promising tool in modern pharmaceutics. The following article describes synthesis of well-defined random and block copolymers by RAFT polymerization with potential medical application. polymers have been labeled positron-emitting nuclide fluorine-18. polymeric structures are based on biocompatible N-(2-hydroxypropyl)-methacrylamide (HPMA). To achieve these structures, functional reactive ester molecular weight within...
Tumor targeting using agents with slow pharmacokinetics represents a major challenge in nuclear imaging and targeted radionuclide therapy as they most often result low contrast high radiation dose to healthy tissue. To address this challenge, we developed polymer-based agent that can be used for pretargeted thus separates tumor accumulation from the step time. The is based on polypeptide-graft-polypeptoid polymers (PeptoBrushes) functionalized trans-cyclooctene (TCO). complementary...
A simple, scalable and reliable direct 18 F-labeling procedure has been developed applied to obtain a pretargeting tetrazine-based imaging agent with favorable in vivo characteristics.
Pretargeted PET imaging is an emerging and fast-developing method to monitor immuno-oncology strategies. Currently, tetrazine ligation considered the most promising bioorthogonal reaction for pretargeting in vivo. Recently, we have developed a 18F-label ultrareactive tetrazines by copper-mediated fluorinations. However, bispyridyl tetrazines-one of structures vivo pretargeted applications-were inaccessible using this strategy. We believed that our successful efforts H-tetrazines low basic...
Tetrazine-trans-cyclooctene ligations are remarkably fast and selective reactions even at low micro-molar concentrations. In bioorthogonal radiochemistry, tools that enable conjugation of radioactive probes to pre-targeted vectors great interest. Herein, we describe the successful development first (11)C-labelled tetrazine its reaction with trans-cyclooctenol.
Pretargeted imaging of nanomedicines have attracted considerable interest because it has the potential to increase contrast while reducing radiation burden healthy tissue. Currently, tetrazine ligation is fastest bioorthogonal reaction for this strategy and, consequently, state-of-art choice in vivo chemistry. We recently identified key properties tetrazines pretargeting. also developed a method 18F-label reactive using an aliphatic nucleophilic substitution strategy. Here, we combined...
The serotonin 7 receptor (5-HT7R) regulates various processes in the central nervous system, including mood, learning, and circadian rhythm control, among others. Receptor activation can lead to of Gαs protein a subsequent increase intracellular cyclic adenosine monophosphate (cAMP). interaction with inverse agonists results decrease basal cAMP levels therefore downstream effect reduced neuronal excitability neurotransmission. Recently, pellotine (1a), Lophophora alkaloid, was unexpectedly...
Pretargeted radioimmunoimaging has been shown to enhance tumor-to-background ratios by up 125-fold at early time points, leading more efficient and less toxic radionuclide therapies, particularly with shorter half-lives such as astatine-211 (211At). The tetrazine ligation is the most utilized bioorthogonal reaction in these strategies, making tetrazines ideal for 211At labeling controlling biodistribution. We developed a 211At-labeled pretargeting agent alpha-radionuclide therapy, achieving...
Pretargeted imaging harnessing tetrazine ligation has gained increased interest over recent years. Targeting vectors with slow pharmacokinetics may be visualized using short-lived radionuclides, such as fluorine-18 (18F) for positron emission tomography (PET), and result in improved target-to-background ratios compared to conventionally radiolabeled slowly accumulating vectors. We recently developed different radiochemical protocols enabling the direct radiofluorination of various scaffolds,...
Tetrazines (Tz) have been applied as bioorthogonal agents for various biomedical applications, including pretargeted imaging approaches. In radioimmunoimaging, pretargeting increases the target-to-background ratio while simultaneously reducing radiation burden. We recently reported a strategy to directly 18F-label highly reactive tetrazines based on 3-(3-fluorophenyl)-Tz core structure. Herein, we report kinetic study this versatile scaffold. A library of 40 different was prepared, fully...