molecules of the month


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

Structure of MGS0274, a potent and selective agonist of mGlu2 and mGlu3 receptors
1 min read

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 cyclopentenone (ref. 9 in article).

request a trial

You don’t have time to read everything, but you can’t afford to fall behind.

Drug Hunter Premium is drug discovery, distilled, so you can quickly catch up and make informed decisions based on industry examples.

Get ahead now by requesting a trial.

already a member? log in: