Sodano, Federica; Lazzarato, Loretta; Rolando, Barbara; Spyrakis, Francesca; De Caro, Carmen; Magliocca, Salvatore; Marabello, Domenica; Chegaev, Konstantin; Gazzano, Elena; Riganti, Chiara; Calignano, Antonio; Russo, Roberto; Rimoli, Maria Grazia published the artcile< Paracetamol-Galactose Conjugate: A Novel Prodrug for an Old Analgesic Drug>, Safety of ((3aR,5R,5aS,8aS,8bR)-2,2,7,7-Tetramethyltetrahydro-3aH-bis([1,3]dioxolo)[4,5-b:4′,5′-d]pyran-5-yl)methanol, the main research area is paracetamol galactose prodrug analgesic; X-ray diffraction; hepatotoxicity; hyperalgesia; metabolism; paracetamol; prodrug.
Paracetamol has been one of the most commonly used and prescribed analgesic drugs for more than a hundred years. Despite being generally well tolerated, it can result in high liver toxicity when administered in specific conditions, such as overdose, or in vulnerable individuals. We have synthesized and characterized a paracetamol galactosylated prodrug (PARgal) with the aim of improving both the pharmacodynamic and pharmacol. profile of paracetamol. PARgal shows a range of physicochem. properties, solubility, lipophilicity, and chem. stability at differing physiol. pH values and in human serum. PARgal could still be preclinically detected 2 h after administration, meaning that it displays reduced hepatic metabolism compared to paracetamol. In overdose conditions, PARgal has not shown any cytotoxic effect in in vitro analyses performed on human liver cells. Furthermore, when tested in an animal pain model, PARgal demonstrated a sustained analgesic effect up to the 12th hour after oral administration. These findings support the use of galactose as a suitable carrier in the development of prodrugs for analgesic treatment.
Molecular Pharmaceutics published new progress about Analgesia. 4064-06-6 belongs to class alcohols-buliding-blocks, and the molecular formula is C12H20O6, Safety of ((3aR,5R,5aS,8aS,8bR)-2,2,7,7-Tetramethyltetrahydro-3aH-bis([1,3]dioxolo)[4,5-b:4′,5′-d]pyran-5-yl)methanol.
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts