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Solute carrier family 12 potassium-chloride transporter member 5 (SLC12A5; KCC2)

In vitro and rat studies suggest stimulating chloride extrusion through KCC2 activation could help treat pain. A high throughput screen of a library of 92,500 drug-like compounds identified KCC2-enhancing agonists. In spinal slices from rats with peripheral nerve injury, the screening hits stimulated KCC2 activity and increased chloride extrusion by 46%. In a rat model of neuropathic pain, the lead KCC2 agonist had analgesic effects comparable to those of Lyrica pregabalin but did not also dampen motor function. Next steps include testing the lead screening hits and their derivatives in models of pain.
Pfizer Inc. markets Lyrica pregabalin to treat multiple neurological conditions including neuropathic pain.

SciBX 6(43); doi:10.1038/scibx.2013.1233
Published online Nov. 7, 2013

Patents for the lead compound and new, undisclosed compounds owned by Laval University; licensing status undisclosed

Gagnon, M. et al. Nat. Med.; published online Oct. 6, 2013;
Contact: Yves De Koninck, Universite Laval, Quebec City,
Quebec, Canada