Multi-parameter optimization: Development of a morpholin-3-one derivative with an improved kinetic profile for imaging monoacylglycerol lipase in the brain

Autor: Yingfang He, Uwe Grether, Marco F. Taddio, Carla Meier, Claudia Keller, Martin R. Edelmann, Michael Honer, Sylwia Huber, Matthias B. Wittwer, Dominik Heer, Hans Richter, Ludovic Collin, Melanie N. Hug, Manuel Hilbert, Annemarieke G.J. Postmus, Anna Floor Stevens, Mario van der Stelt, Stefanie D. Krämer, Roger Schibli, Linjing Mu, Luca C. Gobbi

Publikováno v: European Journal of Medicinal Chemistry, 243:114750. ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
European Journal of Medicinal Chemistry, 243

Monoacylglycerol lipase (MAGL) is a gatekeeper in regulating endocannabinoid signaling and has gained substantial attention as a therapeutic target for neurological disorders. We recently discovered a morpholin-3-one derivative as a novel scaffold fo

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::3e3c55a40e57837b88082305c6a4d833
https://doi.org/10.1016/j.ejmech.2022.114750

Synthesis and Structure-Affinity Relationship of Small Molecules for Imaging Human CD80 by Positron Emission Tomography

Autor: Aristeidis Chiotellis, Tim Gruene, Dominik Schmid, Marco F. Taddio, Roger Schibli, Claudia Adrianna Castro Jaramillo, Stefanie D. Krämer, Simon M. Ametamey, Lukas Muskalla, Linjing Mu, Tanja Bollmann

Publikováno v: Journal of medicinal chemistry. 62(17)

The costimulatory molecule CD80 is an early marker for immune activation. It is upregulated on activated antigen-presenting cells. We aimed at developing a tracer for imaging CD80 by positron emission tomography (PET). Novel CD80 ligands were synthes

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a60563105e1d870fa97417fc9de0c47e
https://pubmed.ncbi.nlm.nih.gov/31430137

Physiologically Based Pharmacokinetic Modelling with Dynamic PET Data to Study the In Vivo Effects of Transporter Inhibition on Hepatobiliary Clearance in Mice

Autor: Marco F. Taddio, Linjing Mu, Claudia Keller, Roger Schibli, Stefanie D. Krämer

Publikováno v: Contrast Media & Molecular Imaging, 2018
Contrast Media & Molecular Imaging, Vol 2018 (2018)

Physiologically based pharmacokinetic modelling (PBPK) is a powerful tool to predict in vivo pharmacokinetics based on physiological parameters and data from in vivo studies and in vitro assays. In vivo PBPK modelling in laboratory animals by noninva

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=dedup_wf_001::1bde0d924360f9f6f733dc5f0bd983f3
https://hdl.handle.net/20.500.11850/274301