Category: pyridine-derivativesIn 2015 ,《Discovery of a High Affinity and Selective Pyridine Analog as a Potential Positron Emission Tomography Imaging Agent for Cannabinoid Type 2 Receptor》 appeared in Journal of Medicinal Chemistry. The author of the article were Slavik, Roger; Grether, Uwe; Muller Herde, Adrienne; Gobbi, Luca; Fingerle, Jurgen; Ullmer, Christoph; Kramer, Stefanie D.; Schibli, Roger; Mu, Linjing; Ametamey, Simon M.. The article conveys some information:
As part of our efforts to develop CB2 PET imaging agents, we investigated 2,5,6-substituted pyridines as a novel class of potential CB2 PET ligands. A total of 21 novel compounds were designed, synthesized, and evaluated for their potency and binding properties toward human and rodent CB1 and CB2. The most promising ligand 6a was radiolabeled with carbon-11 to yield 16 ([11C]RSR-056). Specific binding of 16 to CB2-pos. spleen tissue of rats and mice was demonstrated by in vitro autogadiog. and verified in vivo in PET and biodistribution experiments Furthermore, 16 was evaluated in a lipopolysaccharid (LPS) induced murine model of neuroinflammation. Brain radioactivity was strikingly higher in the LPS-treated mice than the control mice. Compound 16 is a promising radiotracer for imaging CB2 in rodents. It might serve as a tool for the investigation of CB2 receptor expression levels in healthy tissues and different neuroinflammatory disorders in humans. After reading the article, we found that the author used Methyl 5-bromopicolinate(cas: 29682-15-3Category: pyridine-derivatives)
Methyl 5-bromopicolinate(cas: 29682-15-3) belongs to pyridine. The basicity and metallophilic high donor number of these π-deficient systems has long favored them as ligands in metal catalysis. The last decade saw pyridine assume a stronger role as functional group for directed C–H oxidation/activation.Category: pyridine-derivatives