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Sep. 18, 2021

Compound 12: A Selective GluN2B Negative Allosteric Modulator

"compound 12"

selective GluN2B negative allosteric mod. active in brain, proj. oral dose of 120 mg from cell-based HTS and opt. J. Med. Chem., Jul. 31, 2020 Janssen R&D, San Diego, CA

Drug Hunter Team

“compound 12” is a selective negative allosteric modulator of the GluN2B subunit of NDMA receptors intended for treatment of mood disorders. In this program, poor solubility and permeability were a challenge for oral exposure, but was addressed with a nanosuspension formulation. The nanosuspension allowed them to get high enough margins in [...]



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