THERAPY DOSSIER · th-331468868368

Chlormethiazole

Drug · Positive allosteric modulator of the GABA-A receptor anion channel at the barbiturate site; neuroprotective in animal models of global and focal ischaemia

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Evidence & regulatory context

Mechanism: Positive allosteric modulator of the GABA-A receptor anion channel at the barbiturate site; neuroprotective in animal models of global and focal ischaemia
Target: CHEMBL2093872
Injury models: Chemical/toxin
Reported indication: Not recorded
First approval: Not recorded
Development stage: Not recorded
ChEMBL record: CHEMBL315795 ↗
ChEMBL max phase: 4 / 4 (development scale, not regulatory approval)
Synonyms: Chlormethiazole; Clomethiazole; Clometiazol; Distraneurine; Heminevrin
Note: Not recorded

Clinical trials 1

0 linked trials carry an injury-indication flag. These flags support record-level exploration and sit alongside the stringent aggregate counts described in Methods.

NCT02374567 ↗PHASE3terminated

Pharmacovigilance in Gerontopsychiatric Patients (clomethiazole among monitored agents)

Dementia · Depression · Schizophrenia · Anxiety Disorders

Enrolment: 407 · Results not recorded

Preclinical evidence 1

1 studies reported at therapy level; 1 evidence entries itemised.

PMID 24717297 ↗2014Reported benefit

Inhibition of cytochrome P450 2E1 and activation of transcription factor Nrf2 are renoprotective in myoglobinuric acute kidney injury.

RatChemical/toxinSprague-DawleyMale

Model: Glycerol-induced myoglobinuric (rhabdomyolysis) acute kidney injury; LLC-PK1 cells exposed to myoglobin in vitro

Chlormethiazole prevented the rise in renal catalytic iron, reduced oxidative stress, blocked Nrf2 nuclear translocation and haem oxygenase-1 upregulation, and gave functional and histological protection against myoglobinuric acute kidney injury. CYP2E1 inhibition or silencing in tubular epithelial…

Extraction: extract · Supplied extraction confidence: 0.6. Machine-extracted fields require source verification.

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