For research use only. Not for therapeutic Use.
Chlormethiazole is an potent and orally active GABAA agonist[1]. Chlormethiazole inhibits cytochrome P450 isoforms: CYP2A6 and CYP2E1 in human liver microsomes. Chlormethiazole is an anticonvulsant agent and has the potential for treating convulsive status epilepticus[2].
Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents[1].
Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells, with EC50 values of 0.3 and 1.5 mM, respectively[1].
Clomethiazole (30 μM) at low concentration also potentiates the action of GABA in both cell types, equivalent to a 3-fold increase in potency and up to 1.8-fold increase in maximal current[1].
Clomethiazole inhibits cytochrome P450 isoforms, CYP2A6 and CYP2E1 with IC50 values of 24 μM and 42 μM, respectively, in human liver microsomes, meanwhile all other isoforms exhibiting values > 300 μM[2].
| Catalog Number | R018287 |
| CAS Number | 533-45-9 |
| Synonyms | 5-(2-chloroethyl)-4-methyl-1,3-thiazole |
| Molecular Formula | C6H8ClNS |
| Purity | ≥95% |
| InChI | InChI=1S/C6H8ClNS/c1-5-6(2-3-7)9-4-8-5/h4H,2-3H2,1H3 |
| InChIKey | PCLITLDOTJTVDJ-UHFFFAOYSA-N |
| SMILES | CC1=C(SC=N1)CCCl |
| Reference | [1]. Nelson RM, et al.Electrophysiological actions of gamma-aminobutyric acid and clomethiazole on recombinant GABA(A) receptors.Eur J Pharmacol. 2002 Oct 11;452(3):255-62. [2]. Stresser DM, et al. Selective Time- and NADPH-Dependent Inhibition of Human CYP2E1 by Clomethiazole.Drug Metab Dispos. 2016 Aug;44(8):1424-30 |
