Clomethiazole

SKU: orb1308439

Description

Clomethiazole (Distraneurin) is an orally active anticonvulsant and GABAA receptor agonist, researched for potential use in status epilepticus. It is also employed in vitro as a selective inhibitor of human cytochrome P450 isoforms CYP2A6 and CYP2E1 in metabolic studies.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 533-45-9
• MW: 161.65
• Purity: 99.06% (May vary between batches)
• Formula: C₆H₈ClNS
• SMILES: Cl.CC1=C(CCCl)SC=N1
• Target: GABA Receptor,Cytochromes P450
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (30.93 mM);DMSO:240 mg/mL (1484.69 mM)

Bioactivity

• Target IC50:
  CYP2A6/CYP2E1:24 µM and 42 µM
• In Vitro:
  Clomethiazole inhibits cytochrome P450 isoforms, CYP2A6 and CYP2E1 (IC50: 24 μM and 42 μ), in human liver microsomes. But all other isoforms exhibiting values > 300 μM. Clomethiazole (1 mM), in the absence of GABA, to α1/β1/γ2 or α1/β2/γ2 subunit-containing cells produced large whole-cell currents. Clomethiazole activate GABAA currents in α1/β1/γ2- and α1/β2/γ2-containing cells ( EC50: 0.3 and 1.5 mM) . 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

insomnia, Inhibitor, GABAReceptor, GABAA, GABA Receptor, Gamma-aminobutyric acid Receptor, inhibit, neuroprotective, anticonvulsant, alcoholism, 5-(2-CHLOROETHYL)-4-METHYLTHIAZOLE, CYP2E1, CYP2A6, CYPs, Cytochrome P450, Distraneurin, Clomethiazole, Chlormethiazole, sedative, γ-Aminobutyric acid Receptor

Compound Identifiers

PubChem CID

19035073