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Chemical Compound Review

CHEMBL60796     4-[2-[4-[[1-[(4- fluorophenyl)methyl]benzoi...

Synonyms: AG-G-92001, SureCN1152697, CHEBI:191240, CTK8G2140, DNC000539, ...
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Disease relevance of Desmethylastemizole


High impact information on Desmethylastemizole


Chemical compound and disease context of Desmethylastemizole

  • We report the clinical observation of QT prolongation and torsade de pointes in a patient with undetectable serum concentrations of astemizole (< 0.5 ng/ml) and "therapeutic" concentrations of desmethylastemizole (up to 7.7 ng/ml or 17.3 nmol/liter) [1].

Anatomical context of Desmethylastemizole


  1. Torsade de pointes with an antihistamine metabolite: potassium channel blockade with desmethylastemizole. Vorperian, V.R., Zhou, Z., Mohammad, S., Hoon, T.J., Studenik, C., January, C.T. J. Am. Coll. Cardiol. (1996) [Pubmed]
  2. Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole. Zhou, Z., Vorperian, V.R., Gong, Q., Zhang, S., January, C.T. J. Cardiovasc. Electrophysiol. (1999) [Pubmed]
  3. Involvement of CYP2J2 on the intestinal first-pass metabolism of antihistamine drug, astemizole. Matsumoto, S., Hirama, T., Matsubara, T., Nagata, K., Yamazoe, Y. Drug Metab. Dispos. (2002) [Pubmed]
  4. Influence of itraconazole on the pharmacokinetics and electrocardiographic effects of astemizole. Lefebvre, R.A., Van Peer, A., Woestenborghs, R. British journal of clinical pharmacology. (1997) [Pubmed]
  5. Antiallergic effects of major metabolites of astemizole in rats and guinea pigs. Kamei, C., Mio, M., Izushi, K., Kitazumi, K., Tsujimoto, S., Fujisawa, K., Adachi, Y., Tasaka, K. Arzneimittel-Forschung. (1991) [Pubmed]
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