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Sep. 18, 2021

MGS0274: An Oral Prodrug of mGlu2/3 Receptor Agonist


oral prodrug of mGlu2/3 receptor agonist in development for schizophrenia from derivatization of active molecule Eur. J. Med. Chem., Jul. 5, 2020 Taisho Pharmaceutical, Saitama, JP

Drug Hunter Team

MGS0274 is a prodrug of an mGlu2/3 receptor agonist with ca. 15x greater oral exposure than the parent. The ester is believed to be cleaved pre-systemically by liver carboxyesterases to release the innocuous byproducts acetaldehyde, CO2, and menthol. The parent is also an interesting looking molecule prepared in a few steps from [...]



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