The pharmacology and toxicology of meta-substituted acetanilide I: acute toxicity of 3-hydroxyacetanilide in mice

Res Commun Chem Pathol Pharmacol. 1980 Jun;28(3):447-56.


Toxicity of meta or 3-hydroxyacetanilide was evaluated in mice. The LD50 was 1025 mg/kg when given intraperitoneally (i.p.). The drug in doses greater than 400 mg/kg i.p. caused significant sedation. 3-Hydroxyacetanilide, 900 mg/kg i.p., did not cause hepatic necrosis evaluated by either histology or changes in plasma glutamate pyruvate transaminase activity. Acetaminophen (4-hydroxyacetanilide, paracetamol) caused significant liver glutathione depletion two hours after dosing. In contrast, liver glutathione was only slightly decreased by 600 mg/kg i.p. of 3-hydroxyacetanilide at 2 or 4 hours after the dose. It is suggested that the meta-substituted acetanilide derivatives might be safer analgesics and antipyretics than acetaminophen.

MeSH terms

  • Acetaminophen / toxicity*
  • Acetanilides / metabolism
  • Acetanilides / pharmacology
  • Acetanilides / toxicity*
  • Animals
  • Glutathione / analysis
  • Lethal Dose 50
  • Liver / drug effects
  • Liver / pathology
  • Male
  • Mice
  • Transaminases / blood


  • Acetanilides
  • Acetaminophen
  • 3-hydroxyacetanilide
  • Transaminases
  • Glutathione