Competitive GABAA receptor antagonist and also glycine receptor antagonist
REVIEW Thiocolchicoside is a small molecule muscle relaxant and anti-inflammatory agent, shown to function as a competitive gamma-aminobutyric acid type A (GABAA) receptor antagonist. Thiocolchicoside is also shown to inhibit strychnine-sensitive glycine receptors with lower potency than GABAA, and to inhibit human nicotinic acetylcholine receptors with very low relative affinity.
Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010)
Gelmi, M., et al.: J. Med. Chem., 50, 2245 (2007)
Mascia, M., et al.: Eur. J. Pharmacol., 558, 37 (2007)