Synthesis and Pharmacological Evaluation of [11C]4-Methoxy‑N‑[2-(thiophen-2-yl)imidazo[1,2‑a]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ‑Subunit-Containing γ‑Aminobutyric Acid Type A Receptors

Autor: Elina T. L’Estrade, Hanne D. Hansen, Christina Falk-Petersen, Anne Haugaard, Nane Griem-Krey, Sascha Jung, Hartmut Lüddens, Tanja Schirmeister, Maria Erlandsson, Tomas Ohlsson, Gitte M. Knudsen, Matthias M. Herth, Petrine Wellendorph, Bente Frølund

Publikováno v: ACS Omega, Vol 4, Iss 5, Pp 8846-8851 (2019)

Externí odkaz: https://doaj.org/article/bd6775d756734cf4926d9d3fcbed21d7

In Vitro and In Vivo Characterization of Dibenzothiophene Derivatives [125I]Iodo-ASEM and [18F]ASEM as Radiotracers of Homo- and Heteromeric α7 Nicotinic Acetylcholine Receptors

Autor: Cornelius K. Donat, Henrik H. Hansen, Hanne D. Hansen, Ronnie C. Mease, Andrew G. Horti, Martin G. Pomper, Elina T. L’Estrade, Matthias M. Herth, Dan Peters, Gitte M. Knudsen, Jens D. Mikkelsen

Publikováno v: Molecules, Vol 25, Iss 6, p 1425 (2020)

The α7 nicotinic acetylcholine receptor (α7 nAChR) is involved in several cognitive and physiologic processes; its expression levels and patterns change in neurologic and psychiatric diseases, such as schizophrenia and Alzheimer’s disease, which

Externí odkaz: https://doaj.org/article/efc1f66ada2543bca63ea2541a8178d8

In Vivo Veritas: 18F-Radiolabeled Glycomimetics Allow Insights into the Pharmacological Fate of Galectin-3 Inhibitors

Autor: Fredrik Zetterberg, Kristoffer Peterson, Edvard Torkelsson, Maria Erlandsson, Nic Gillings, Vladimir Shalgunov, Hakon Leffler, Tomas G Olsson, Mengfei Xiong, Matthias M. Herth, Ulf J. Nilsson, Klas Bratteby, Elina T. L’Estrade

Publikováno v: Journal of Medicinal Chemistry. 63:747-755

Glycomimetic drugs have attracted increasing interest as unique targeting vectors or surrogates for endogenous biomolecules. However, it is generally difficult to determine the in vivo pharmacokinetic profile of these compounds. In this work, two gal

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::0cd311416633749e1f81029303072a17
https://doi.org/10.1021/acs.jmedchem.9b01692

Synthesis and Pharmacological Evaluation of [11C]4-Methoxy-N-[2-(thiophen-2-yl)imidazo[1,2-a]pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the δ-Subunit-Containing γ-Aminobutyric Acid Type A Receptors

Autor: Sascha Jung, Petrine Wellendorph, Gitte M. Knudsen, Anne S. Haugaard, Elina T. L’Estrade, Christina Birkedahl Falk-Petersen, Bente Frølund, Matthias M. Herth, Nane Griem-Krey, Tomas Ohlsson, Maria Erlandsson, Hartmut Lüddens, Tanja Schirmeister, Hanne D. Hansen

Publikováno v: ACS Omega, Vol 4, Iss 5, Pp 8846-8851 (2019)
L'Estrade, E T, Hansen, H D, Falk-Petersen, C, Haugaard, A, Griem-Krey, N, Jung, S, Lueddens, H, Schirmeister, T, Erlandsson, M, Ohlsson, T, Knudsen, G M, Herth, M M, Wellendorph, P & Frolund, B 2019, ' Synthesis and Pharmacological Evaluation of [C-11]4-Methoxy-N-[2-(thiophen-2-yl) imidazo[1,2-a] pyridin-3-yl]benzamide as a Brain Penetrant PET Ligand Selective for the delta-Subunit-Containing gamma-Aminobutyric Acid Type A Receptors ', ACS Omega, vol. 4, no. 5, pp. 8846-8851 . https://doi.org/10.1021/acsomega.9b00434

The α4/6βδ-containing GABAA receptors are involved in a number of brain diseases. Despite the potential of a δ-selective imaging agent, no PET radioligand is currently available for in vivo imaging...

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2e74f11686ca51dc163709601bff82f
https://doi.org/10.1021/acsomega.9b00434

Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of [18F]ENL30: A Potential PET Radiotracer for the 5‑HT7 Receptor

Autor: Simone L. Baerentzen, Maria Erlandsson, Vladimir Shalgunov, Mengfei Xiong, Elina T. L’Estrade, Mikael Palner, Gitte M. Knudsen, Fraser G. Edgar, Tomas Ohlsson, Matthias M. Herth

Publikováno v: ACS Omega, Vol 4, Iss 4, Pp 7344-7353 (2019)
Tampio L'Estrade, E, Edgar, F G, Xiong, M, Shalgunov, V, Baerentzen, S L, Erlandsson, M, Ohlsson, T G, Palner, M, Knudsen, G M & Herth, M M 2019, ' Synthesis, Radiolabeling, and in Vitro and in Vivo Evaluation of [ 18 F]ENL30 : A Potential PET Radiotracer for the 5-HT 7 Receptor ', ACS Omega, vol. 4, no. 4, pp. 7344-7353 . https://doi.org/10.1021/acsomega.9b00394

The 5-HT 7 receptor (5-HT 7 R) is involved in a broad range of physiological conditions and disorders. Currently, there is no validated clinical positron emission tomography (PET) tracer available; however, we have recently developed a promising 11 C

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8ee8b6904a2004110d014fb2a6689667
https://doaj.org/article/a2f7493d2aa241d4aaf74d2a67c30505