Featured Paper of the Month – December 2015
Published in The Journal of Medical Chemistry by Selfridge, Brandon R; Wang, Xiaohui; Zhang, Yingning; Yin, Hang; Grace, Peter M; Watkins, Linda R; Jacobson, Arthur E; Rice, Kenner C
Activation of Toll-like receptors has been linked to neuropathic pain and opioid dependence. (+)-Naltrexone acts as a Toll-like receptor 4 (TLR4) antagonist and has been shown to reverse neuropathic pain in rat studies. We designed and synthesized compounds based on (+)-naltrexone and (+)-noroxymorphone and evaluated their TLR4 antagonist activities by their effects on inhibiting lipopolysaccharide (LPS) induced TLR4 downstream nitric oxide (NO) production in microglia BV-2 cells…