Block the road of pain

Neurons of pain receptors transmit signals to the brain using ion streams generated by sodium channels and controlled by charge; in the case of osteoarthritis and other pain syndromes, the channels are usually in a state of hyperactivity. The research group of Paul Deken from Northwestern University suggested that blocking the flow of ions can be used as a method of anesthesia for osteoarthritis.

Previously, Deken and colleagues demonstrated that a derivative of tamoxifen – an estrogen receptor modulator – binds to the intracellular gates of sodium channels. In the new study, they injected the tamoxifen metabolite into mice genetically modified to develop osteoarthritis symptoms.

Schematic representation of the Nav1.7 sodium channel blocked by the tamoxifen metabolite ND-Tam. The potentials of action of nociceptors responsible for the transmission of pain signals are reduced.

The researchers found that the drug binds to two sites of intracellular receptors in sodium channels, blocking the flow of ions in hyperactive neurons of pain receptors responsible for pain in osteoarthritis.

The clinical efficacy of tamoxifen metabolites for the treatment of pain syndrome in osteoarthritis has not yet been studied. Nevertheless, long-term data on the use of the drug in oncological practice greatly simplify its study and can reduce the overall development costs for use in osteoarthritis.

Article by M.M.McCollum et al. Targeting the tamoxifen receptor within sodium channels to block osteoarthritic pain is published in the journal Cell Reports.

Aminat Adzhieva, portal "Eternal Youth" http://vechnayamolodost.ru based on materials from Northwestern University: Targeting Ion Channels to Manage Osteoarthritis Pain.