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The σ1 receptor engages the redox-regulated HINT1 protein to bring opioid analgesia under NMDA receptor negative control.

Antioxid Redox Signal.. 2015-03;  22(10):799-818
Rodriguez-Munoz M, Sanchez-Blazquez P, Herrero-Labrador R, Martinez-Murillo R, Merlos M, Vela JM, GarzÓn J. NeurofarmacologÍa, Instituto Cajal, Consejo Superior de Investigaciones CientÍficas (CSIC), Madrid, Spain.
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摘要

Aims: The in vivo pharmacology of the sigma 1 receptor (σ1R) is certainly complex; however, σ1R antagonists are of therapeutic interest because they enhance mu-opioid receptor (MOR)-mediated antinociception and reduce neuropathic pain. Thus, we investigated whether the σ1R is involved in the negative control that glutamate N-methyl-D-aspartate receptors (NMDARs) exert on opioid antinociception. Results: A redox-regulated process situates MOR signaling under NMDAR control, and in this context, the σ1R binds to the cytosolic C terminal region of the NMDAR NR1 subunit. The MOR C terminus carries the histidine triad nucleotide-binding protein 1 (HINT1) coupled to the regulator of G-protein s... More

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