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KI1413Clomethiazole250 mg$250

Chemical Characteristic

Product NameClomethiazole
SynonymsChlormethiazole, Heminevrin
CAS No.533-45-9
Molecular Weight 161.65
FormulaC6H8ClNS
Chemical Name5-(2-Chloroethyl)-4-methylthiazole
Smiless1cnc(c1CCCl)C
Chemical Structure

Biological activities

Chlomethiazole is a positive GABAA receptor allosteric modulator. Chlomethiazole is used in treating and preventing symptoms of acute alcohol withdrawal. Clomethiazole prevents ischaemia-triggered glutamate efflux with an IC50 of 24 µM.[1] However, it is reported that clomethiazole does not affect cycles of cortical spreading depression.[2] Chlomethiazole decreases the inflammatory response in experimental extracorporeal circulation.[3] Compared to saline-treated injured animals, chlomethiazole increases grey matter by 16%.[4]

Protocols

In vivo: Clomethiazole (100 mg/kg) is dissolved in 0.9% NaCl solution.[2]

References

[1] Nelson RM, et al. On the regulation of ischaemia-induced glutamate efflux from rat cortex by GABA; in vitro studies with GABA, clomethiazole and pentobarbitone. Br J Pharmacol. 2000, 130(5):1124-1130.
[2] Addae JI, et al. Effects of AMPA and clomethiazole on spreading depression cycles in the rat neocortex in vivo. Eur J Pharmacol. 2011, 653(1-3): 41-46.
[3] Harmon D, et al. The effect of clomethiazole on plasma concentrations of interleukin-6, -8, -1beta, tumor necrosis factor-alpha, and neutrophil adhesion molecule expression during experimental extracorporeal circulation.Anesth Analg. 2003, 97(1): 13-18.
[4] Farooque M, et al. Clomethiazole (ZENDRA, CMZ) improves hind limb motor function and reduces neuronal damage after severe spinal cord injury in rat. Acta Neuropathol. 1999, 98(1): 22-30.

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