99424-76-7Relevant academic research and scientific papers
Synthesis and Biological Evaluation of Endocannabinoid Uptake Inhibitors Derived from WOBE437
M?der, Patrick,Bartholom?us, Ruben,Nicolussi, Simon,Baumann, Alice,Weis, Melanie,Chicca, Andrea,Rau, Mark,Sim?o, Ana Catarina,Gertsch, Jürg,Altmann, Karl-Heinz
, p. 145 - 154 (2020/06/02)
WOBE437 ((2E,4E)-N-(3,4-dimethoxyphenethyl)dodeca-2,4-dienamide, 1) is a natural product-derived, highly potent inhibitor of endocannabinoid reuptake. In this study, we synthesized almost 80 analogues of 1 with different types of modifications in the dodecadienoyl domain as well as the dimethoxyphenylethyl head group, and we investigated their effects on anandamide uptake into U937 cells. Intriguingly, none of these analogues was a more potent inhibitor of anandamide uptake than WOBE437 (1). At the same time, a number of WOBE437 variants exhibited potencies in the sub-100 nM range, with high selectivity over inhibition of the endocannabinoid-degrading enzyme fatty acid amide hydrolase; two compounds were virtually equipotent with 1. Interestingly, profound activity differences were observed between analogues in which either of the two methoxy substituents in the head group had been replaced by the same bulkier alkoxy group. Some of the compounds described here could be interesting departure points for the development of potent endocannabinoid uptake inhibitors with more drug-like properties.
Enhanced copper-mediated 18F-fluorination of aryl boronic esters provides eight radiotracers for PET applications
Preshlock, Sean,Calderwood, Samuel,Verhoog, Stefan,Tredwell, Matthew,Huiban, Mickael,Hienzsch, Antje,Gruber, Stefan,Wilson, Thomas C.,Taylor, Nicholas J.,Cailly, Thomas,Schedler, Michael,Collier, Thomas Lee,Passchier, Jan,Smits, René,Mollitor, Jan,Hoepping, Alexander,Mueller, Marco,Genicot, Christophe,Mercier, Jo?l,Gouverneur, Véronique
supporting information, p. 8361 - 8364 (2016/07/07)
[18F]FMTEB, [18F]FPEB, [18F]flumazenil, [18F]DAA1106, [18F]MFBG, [18F]FDOPA, [18F]FMT and [18F]FDA are prepared from the corresponding arylboronic esters and [18
Radiofluorinated N-Octanoyl Dopamine ([18F]F-NOD) as a Tool to Study Tissue Distribution and Elimination of NOD in Vitro and in Vivo
Pretze, Marc,Pallavi, Prama,Roscher, Mareike,Klotz, Sarah,Caballero, Julio,Binzen, Uta,Greffrath, Wolfgang,Treede, Rolf-Detlef,Harmsen, Martin C.,Hafner, Mathias,Yard, Benito,W?ngler, Carmen,W?ngler, Bj?rn
, p. 9855 - 9865 (2016/11/19)
To mitigate pretransplantation injury in organs of potential donors, N-octanoyl dopamine (NOD) treatment might be considered as it does not affect hemodynamic parameters in braindead (BD) donors. To better assess optimal NOD concentrations for donor treat
SYNTHESIS AND HPLC SEPARATION OF 6-FLUORO-L-DOPA METABOLITES
Luxen, A.,Monclus, M.,Hendrickx, P.-Y.,Masson, C.,Melega, W. P.
, p. 217 - 226 (2007/10/02)
The synthesis of 6-fluoro-L-dopa metabolites (3-O-methyl-6-fluorodopa (1b), 6-fluorodopamine (2a), 3-O-methyl-6-fluorodopamine (2b), 3,4-dihydroxy-6-fluorophenylacetic acid (3a) and 6-fluorohomovanillic acid (3b) is described.A HPLC method for their separ
