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Chlormezanone (Trancopal)，a non-benzodiazepine that is used in the management of anxiety. It has been suggested for use in the treatment of muscle spasm. Chlormezanone binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.
| Molecular Weight | 273.74 |
| Formula | C11H12ClNO3S |
| CAS Number | 80-77-3 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Marianne Lerch, et al. Current Perspectives on Erythema Multiforme
[3] P Netter, et al. Diclofenac sodium-chlormezanone poisoning
| Related GABA Receptor Products |
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| β-CCB
β-CCB is a ligand for benzodiazepine receptor, which inhibits the binding of [3H]flunitrazepam and ethyl (3-[3H]carboline-3-carboxylate to benzodiazepine receptors, with Ki of 3-4 nM. |
| TPMPA
TPMPA, a hybrid of isoguvacine and 3-APMPA, is the first selective antagonist for a GABAC receptor (KB = 2.1 μM), but not to interact with GABAA (KB = 320 μM) or GABAB receptors (EC50 = 500 μM). |
| CI-966
CI-966 is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. |
| NCS-382
NCS-382 is a potent GABA receptor antagonist and also a GHBR receptor antagonist. |
| CGS 8216
CGS 8216, a benzodiazepine receptor antagonist, inhibits 3H-flunitrazepam (3H-FLU) binding to rat synaptosomal membranes in vitro at subnanomolar concentrations. |
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