BioCentury
ARTICLE | Distillery Therapeutics

Neurology

January 18, 2017 8:49 PM UTC

Cell culture and mouse studies identified a positive allosteric modulator (PAM) of GLRA3 that could help treat neuropathic pain. High throughput screening and chemical synthesis to optimize hits yielded a tricyclic sulfonamide-based GLRA3 PAM that increased analgesia-related glycine-induced synaptic currents in mouse spinal cord slices compared with no treatment. In a mouse model of injury-induced neuropathic pain, the compound decreased mechanical allodynia with potency comparable to Lyrica pregabalin. Next steps by Amgen Inc. could include testing the compound in other models of neuropathic pain (see “Pockets Against Pain”)...

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Amgen Inc.