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)
  • 발행 : 2002.10.01

초록

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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