Bioactivation of the cannabinoid receptor antagonist rimonabant to a cytotoxic iminium ion metabolite.

Foster, Alison J; Prime, Lucy H; Gustafsson, Frida; Temesi, David G; Isin, Emre M; Midlöv, Johanna; Castagnoli, Neal; Kenna, J Gerry

Foster, Alison J; Prime, Lucy H; Gustafsson, Frida; Temesi, David G; Isin, Emre M; Midlöv, Johanna; Castagnoli, Neal; Kenna, J Gerry.

Affiliation

Foster AJ; Global Safety Assessment, DMPK Innovative Medicine, AstraZeneca , Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom.

Chem Res Toxicol ; 26(1): 124-35, 2013 Jan 18.

Article in En | MEDLINE | ID: mdl-23234359

Subject(s)

Cannabinoid Receptor Antagonists/chemistry; Imines/chemistry; Piperidines/chemistry; Pyrazoles/chemistry; Cannabinoid Receptor Antagonists/metabolism; Cannabinoid Receptor Antagonists/toxicity; Carbon Radioisotopes/chemistry; Cell Line, Transformed; Cell Survival/drug effects; Cytochrome P-450 Enzyme System/chemistry; Cytochrome P-450 Enzyme System/metabolism; Glutathione/metabolism; Humans; Ions/chemistry; Metabolome/drug effects; Piperidines/metabolism; Piperidines/pharmacology; Piperidines/toxicity; Potassium Cyanide/chemistry; Potassium Cyanide/pharmacology; Protein Binding; Proteins/chemistry; Proteins/metabolism; Pyrazoles/metabolism; Pyrazoles/toxicity; Rimonabant; Ritonavir/chemistry; Ritonavir/pharmacology

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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Piperidines / Pyrazoles / Cannabinoid Receptor Antagonists / Imines Limits: Humans Language: En Journal: Chem Res Toxicol Journal subject: TOXICOLOGIA Year: 2013 Type: Article Affiliation country: United kingdom

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