Schinina, Barbara; Martorana, Andrea; Colabufo, Nicola Antonio; Contino, Marialessandra; Niso, Mauro; Perrone, Maria Grazia; De Guidi, Guido; Catalfo, Alfio; Rappazzo, Giancarlo; Zuccarello, Elisa; Prezzavento, Orazio; Amata, Emanuele; Rescifina, Antonio; Marrazzo, Agostino published an article in 2015, the title of the article was 4-Nitro-2,1,3-benzoxadiazole derivatives as potential fluorescent sigma receptor probes.Product Details of 39512-49-7 And the article contains the following content:
New fluorescent derivatives for σ receptors were designed and synthesized. To achieve this purpose, a 4-nitro-2,1,3-benzoxadiazole fluorescent tag was connected through a piperazine linker to a modified skeleton derived from selected σ receptor agonists or antagonists. Compounds 5g, 7b, 7e and 7g displayed high σ1 affinity and low σ1/σ2 selectivity (Kiσ1 ranging from 31.6 nM to 48.5 nM, Kiσ1/σ2 = 5-18), while compound 5d exhibited high σ2 affinity and selectivity (Kiσ2 = 56.8 nM, Kiσ1 > 5000 nM). Binding affinity studies revealed that compounds 5d, 5g, 7b, 7e and 7g showed no affinity towards several receptors including opioid, dopaminergic, serotonergic, adrenergic, muscarinic, histaminergic, N-methyl-D-aspartate (NMDA), NMDA receptor channel, or dopamine and serotonin transporters. The fluorescent properties, cellular uptake and confocal microscopy studies on 5d suggest a potential use of this probe to further clarify the mol. role of σ2 receptor subtypes in normal and cancer cells. The experimental process involved the reaction of 4-(4-Chlorophenyl)piperidin-4-ol(cas: 39512-49-7).Product Details of 39512-49-7
The Article related to benzoxadiazole derivative sigma receptor probe, Biochemical Methods: Synthesis and other aspects.Product Details of 39512-49-7
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