• DOI:10.1006/BBRC.1993.1761
• Corpus ID: 21821604

Involvement of CYP2D6 in oxidative metabolism of cinnarizine and flunarizine in human liver microsomes.

@article{Narimatsu1993InvolvementOC,
  title={Involvement of CYP2D6 in oxidative metabolism of cinnarizine and flunarizine in human liver microsomes.},
  author={Shizuo Narimatsu and Satoru Kariya and S Isozaki and Shigeru Ohmori and Mitsukazu Kitada and Shunji Hosokawa and Yasuhiro Masubuchi and T. Suzuki},
  journal={Biochemical and biophysical research communications},
  year={1993},
  volume={193 3},
  pages={
          1262-8
        }
}

• S. Narimatsu, S. Kariya, +5 authors T. Suzuki
• Published 30 June 1993
• Chemistry, Biology
• Biochemical and biophysical research communications

Oxidative metabolism of cinnarizine (CZ) and its fluorine derivative flunarizine (FZ), both of which are selective calcium entry blockers, was examined in human liver microsomes. The ring-hydroxylations and the N-desalkylations constituted primary metabolic pathways in microsomal metabolism of CZ and FZ. Among these pathways, the ring-hydroxylase (p-hydroxylation) activities at the cinnamyl moiety of both drugs were highly correlated with debrisoquine 4-hydroxylase activity and CYP2D6 content. Quinidine, a selective inhibitor of CYP2D6, suppressed the ring-hydroxylase activities of CZ and FZ. These results suggest that CYP2D6 is involved in the ring-hydroxylation of the cinnamyl moiety of both CZ and FZ in human liver microsomes.