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Brain Res. 2011 Jan 25;1370:34-42. doi: 10.1016/j.brainres.2010.11.038. Epub 2010 Dec 4.

Effects of minocycline on Na+ currents in rat dorsal root ganglion neurons.

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Department of Pharmacology, College of Medicine, Chung-Ang University, Seoul 156-756, Republic of Korea.


Minocycline is an inhibitor of microglial activation and proliferation. Minocycline suppresses pain-related behaviors in many different pain states, which correlates closely with its inhibition of microglial activation and subsequent release of pro-inflammatory mediators in the spinal cord. Na(+) channels in dorsal root ganglion (DRG) neurons are implicated in the generation of inflammatory and neuropathic pain. To elucidate a possible peripheral mechanism of minocycline analgesia, effects of minocycline on tetrodotoxin-sensitive and tetrodotoxin-resistant Na(+) currents in rat DRG neurons were investigated. Minocycline potently inhibited both types of Na(+) currents with IC(50) values of 350 nM and 410 nM, respectively. The inhibition was accompanied by a depolarizing shift of the activation voltage. However, minocycline slowed the inactivation and speeded up the recovery from inactivation. These results suggest minocycline may exert analgesia peripherally thorough Na(+) channel inhibition in the primary afferent neurons as well as centrally through microglial inhibition in the spinal cord.

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