The pharmacology and toxicology of meta-substituted acetanilide I: acute toxicity of 3-hydroxyacetanilide in mice.
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.
D000082:Acetaminophen / Q000633:toxicity*; D000083:Acetanilides / Q000378:metabolism / Q000494:pharmacology / Q000633:toxicity*; D000818:Animals; D005978:Glutathione / Q000032:analysis; D007928:Lethal Dose 50; D008099:Liver / Q000187:drug effects / Q000473:pathology; D008297:Male; D051379:Mice; D000637:Transaminases / Q000097:blood
D000083:Acetanilides; D000082:Acetaminophen; C026137:3-hydroxyacetanilide; D000637:Transaminases; D005978:Glutathione