In 2018,Cooper, Anna G.; Oyagawa, Caitlin R. M.; Manning, Jamie J.; Singh, Sameek; Hook, Sarah; Grimsey, Natasha L.; Glass, Michelle; Tyndall, Joel D. A.; Vernall, Andrea J. published ãDevelopment of selective, fluorescent cannabinoid type 2 receptor ligands based on a 1,8-naphthyridin-2-(1H)-one-3-carboxamide scaffoldã?MedChemComm published the findings.Related Products of 27489-62-9 The information in the text is summarized as follows:
Cannabinoid type 2 (CB2) receptor has been implicated in several diseases and conditions, however no CB2 receptor selective drugs have made it to market. The aim of this study was to develop fluorescent ligands as CB2 receptor tools, to enable an increased understanding of CB2 receptor expression and signalling and thereby accelerate drug discovery. Fluorescent ligands have been successfully developed for other receptors, however none with adequate subtype selectivity or imaging properties have been reported for CB2 receptor. A series of 1,8-naphthyridin-2-(1H)-one-3-carboxamides with linkers and fluorophores appended in the N1 and C3-positions were developed. Mol. modeling indicated the C3 cis-cyclohexanol-linked compounds directed the linker out of the CB2 receptor between transmembrane helixes 1 and 7. Herein we report fluorescent ligand 32 (hCB2 pKi = 6.33 ± 0.02) as one of the highest affinity, selective CB2 receptor fluorescent ligands reported. Despite 32 displaying poor specific labeling of CB2 receptor, the naphthyridine scaffold with this linker remains highly promising for future development of CB2 receptor tools. The experimental part of the paper was very detailed, including the reaction process of trans-4-Aminocyclohexanol(cas: 27489-62-9Related Products of 27489-62-9)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.Related Products of 27489-62-9
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