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Chemical Compound Review: 

CTK1A3014     6-[4-(3,4- dimethoxyphenyl)carbonyl- 2,3...

Synonyms: OPC 18692, AC1MJ0S7, 211369-52-7
 
 
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Disease relevance of OPC 18692

  • Vesnarinone, a positive inotropic drug developed for congestive heart failure, and its metabolites (OPC-8230, OPC-18136, OPC-18137) were analyzed in human dialysate and urine (plus an additional metabolite: OPC-18692 in urine) samples using a modification to a previously published LC-MS/MS assay for the analysis of human plasma and urine samples [1].
 

High impact information on OPC 18692

  • OBJECTIVE: To identify the cytochrome P450 (CYP) enzymes involved in the conversion of vesnarinone to it main primary metabolite OPC-18692 and to investigate the effect of CYP3A inhibition on the pharmacokinetics of vesnarinone in vivo [2].
  • The results indicate that CYP2E1 inhibition has only a modest, clinically insignificant effect on vesnarinone disposition but markedly increases plasma concentrations of the OPC-18692 metabolite [3].

References

  1. Extended application of an LC-MS/MS method for the analysis of vesnarinone and its metabolites in human urine and dialysate fluid. Sekar, K.S., Bramer, S.L. Journal of pharmaceutical and biomedical analysis. (2003) [Pubmed]
  2. Effect of CYP3A inhibition on vesnarinone metabolism in humans. Wandel, C., Lang, C.C., Cowart, D.C., Girard, A.F., Bramer, S., Flockhart, D.A., Wood, A.J. Clin. Pharmacol. Ther. (1998) [Pubmed]
  3. Effect of disulfiram-mediated CYP2E1 inhibition on the disposition of vesnarinone. Frye, R.F., Tammara, B., Cowart, T.D., Bramer, S.L. Journal of clinical pharmacology. (1999) [Pubmed]
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