ãDesign and Synthesis of Fluorescent Methylphenidate Analogues for a FRET-Based Assay of Synapsin III Bindingã?was written by Casiraghi, Andrea; Longhena, Francesca; Straniero, Valentina; Faustini, Gaia; Newman, Amy H.; Bellucci, Arianna; Valoti, Ermanno. Category: alcohols-buliding-blocks And the article was included in ChemMedChem in 2020. The article conveys some information:
The authors previously described synapsin III (Syn III) as a synaptic phosphoprotein that controls dopamine release in cooperation with α-synuclein (aSyn). Moreover, in Parkinson’s disease (PD), Syn III also participates in aSyn aggregation and toxicity. The authors’ recent observations point to threo-methylphenidate (MPH), a monoamine re-uptake inhibitor that efficiently counteracts the freezing-gait characteristic of advanced PD, as a ligand for Syn III. The authors have designed and synthesized two different fluorescently labeled MPH derivatives, one with Rhodamine Red (RHOD) and one with 5-carboxytetramethylrhodamine (TAMRA), to be used for assessing MPH binding to Syn III by FRET. TAMRA-MPH exhibited the ideal characteristics to be used as a FRET acceptor, as it was able to enter into the SK-N-SH cells and could interact specifically with human green fluorescent protein (GFP)-tagged Syn III but not with GFP alone. Moreover, the uptake of TAMRA-MPH and co-localization with Syn III was also observed in primary mesencephalic neurons. These findings support that MPH is a Syn III ligand and that TAMRA-conjugated drug mols. might be valuable tools to study drug-ligand interactions by FRET or to detect Syn III in cytol. and histol. samples. In addition to this study using 4-Aminobutan-1-ol, there are many other studies that have used 4-Aminobutan-1-ol(cas: 13325-10-5Category: alcohols-buliding-blocks) was used in this study.
4-Aminobutan-1-ol(cas: 13325-10-5) is used in the synthesis of NSAIDs with anti-inflammatory properties. Also used in the synthesis of polyamine transport ligands with specificity against human cancers allowing easy access to specific cancer cells.Category: alcohols-buliding-blocks
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