Overview
Alternative Name Somnevrin hydrochloride
Lyophilized Powder yes
Source Synthetic
MW: 198.11
Purity: >96%
Effective concentration 0.01-1 mM.
Structure
Chemical name 5-(2-chloroethyl)-4-methyl-1,3-thiazole;hydrochloride.
Molecular formula C6H9Cl2NS.
CAS No.: 6001-74-7
PubChem CID 19035073
Activity Chlormethiazole both directly activates GABAA receptors (at 0.3 – 1 mM), and potentiates GABA-induced activation at various GABAA receptor subtypes (with EC50 of 20 – 160 µM)1. It was also shown to potentiate glycine-induced currents in both bovine chromaffin cells and murine spinal neurons (at 100 µM)2.
References-Activity
- Usala, M. et al. (2003) Br. J. Pharmacol. 140, 1045.
- Hales, T.G. and Lambert, J.J. (1992) Eur. J. Pharmacol. 210, 239.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored desiccated at -20°C.
Solubility Up to 200 mM in H2O. Centrifuge all product preparations before use (10000 x g 5 min).
Storage of solutions Up to four weeks at 4°C or three months at -20°C. It is recommended to aliquot reconstituted product for storage.
Our bioassay
Alomone Labs Chlormethiazole hydrochloride activates GABA(A) receptors expressed in Xenopus oocytes.Time course of GABA(A) α1/β2 currents, directly activated by 0.25 mM and 1 mM Chlormethiazole hydrochloride (#C-360), reversibly and in a concentration-dependent manner, while membrane potential was held at -60 mV.
Scientific background
Chlormethiazole hydrochloride, a thiazole derivative, is a sedative, hypnotic and anxiolytic compound that has been used for the treatment of alcohol-withdrawal symptoms, status epilepticus and pre-eclampsia.
Chlormethiazole acts as a positive modulator of GABA(A) and glycine receptors and holds structural similarity to the β-subunit-selective compound loreclezole. In several studies, the compound was also shown to have neuroprotective properties in models of ischaemia1,2,3.
GABA(A) receptors are members of the Cys-loop superfamily of ligand-gated ion channels and mediate GABA action, a major inhibitory neurotransmitter, throughout the central nervous system. GABA(A) receptors are considered to be a major target of antiseizure drugs4.
Target GABA(A), Glycine receptors
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
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