Thiocolchicoside is a GABAA receptor antagonist.1 It inhibits GABAA receptor-mediated currents in Purkinje cells isolated from rat cerebellum (IC50 = 0.15 ?M). It binds strychnine-sensitive glycine receptors in isolated rat spinal cord (IC50 = 1.58 ?M).2 Thiocolchicoside inhibits cell growth in a panel of cancer cell lines, including KBM5 leukemia and U266 myeloma cells, SCC4 squamous cell carcinoma cells, and HCT116 colon, MCF-7 breast, and A293 kidney cancer cells when used at concentrations ranging from 25 to 100 ?M.3 It inhibits the anti-apoptotic proteins Bcl-2, X-linked inhibitor of apoptosis (XIAP), myeloid cell leukemia-1 (Mcl-1), Bcl-xL, cIAP-1, and cIAP-2 in KBM5 cells in a concentration-dependent manner. It also inhibits TNF-α-induced NF-κB activation and IκBα degradation in KBM5 cells in a concentration-dependent manner. Formulations containing thiocolchicoside have been used as muscle relaxers in the treatment of rheumatoid arthritis, joint stiffness, and muscle stiffness.
1.Carta, M., Murru, L., Botta, P., et al.The muscle relaxant thiocolchicoside is an antagonist of GABAA receptor function in the central nervous systemNeuropharmacology51(4)805-815(2006) 2.Cimino, M., Marini, P., and Cattabeni, F.Interaction of thiocolchicoside with [3H]strychnine binding sites in rat x spinal cord and brainstemEur. J. Pharmacol.318(1)201-204(1996) 3.Reuter, S., Prasad, S., Phromnoi, K., et al.Thiocolchicoside exhibits anticancer effects through downregulation of NF-κB pathway and its regulated gene products linked to inflammation and cancerCancer Prev. Res. (Phila)3(11)1462-1472(2010)