Selectivity of the optical isomers of KR30031 on MDR reversal activity and cardiotoxicity

  • Lee, Byung-Ho (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Lee, Chong-Ock (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Kwon, Myung-Ja (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Yi, Kyu-Yang (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Yoo, Sung-Eun (Medicinal Science Division, Korea Research Institute of Chemical Technology) ;
  • Choi, Sang-Un (Medicinal Science Division, Korea Research Institute of Chemical Technology)
  • Published : 2002.10.01

Abstract

The present study was performed to compare the cardiovascular adverse effects of verapamil. KR30031 and their each optical isomers, and also to measure their ability to overcome multidrug resistance (MDR). R-isomer of KR30031 (R-KR30031) was equipotent with S-isomer of KR30031 (S-KR30031) and 25 fold less potent than R-isomer of verapamil (R-verapamil) in relaxing the aorta isolated from rat (EC50: 11.8, 10.2 and 0.46 ${\mu}$M, respectively). (omitted)

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