Interaction between Bay-K-8644 and various relaxant agents on K+-depolarized contracture of guinea pig taenia coli

Gen Pharmacol. 1988;19(1):113-6. doi: 10.1016/0306-3623(88)90015-8.

Abstract

1. Interaction between Bay-K-8644 and nifedipine, D600, diltiazem, papaverine or W-7 on a K+-contracture of the guinea pig taenia coli have been investigated. 2. These relaxing drugs except Bay-K-8644 inhibited the K+-contracture in a concentration-dependent manner. 3. Complete inhibition by nifedipine (1 x 10(-7) M) of the contracture was absolutely antagonized by Bay-K-8644 (1 x 10(-6) M), a Ca2+-agonist, an apparent pA2 value of Bay-K-8644 as an antagonist for nifedipine obtained from Schild plot being 7.94 and its slope 0.99. 4. Marked inhibitions by D600 (1 x 10(-5) M), diltiazem (1 x 10(-5) M), papaverine (1 x 10(-4) M) and W-7 (1 x 10(-4) M) were unaffected but mild inhibitions by around IC50 of these relaxing agents, except W-7, were fully antagonized by Bay-K-8644. 5. These results suggest that Bay-K-8644 is a competitive antagonist for nifedipine, but not for other agents, on common Ca2+ channel sites.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester / pharmacology*
  • Animals
  • Colon / drug effects
  • Dihydropyridines / pharmacology
  • Diltiazem / pharmacology
  • Ethanol / pharmacology
  • Gallopamil / pharmacology
  • Guinea Pigs
  • In Vitro Techniques
  • Male
  • Muscle Contraction / drug effects
  • Muscle Relaxants, Central / pharmacology*
  • Muscle, Smooth / drug effects*
  • Nifedipine / pharmacology
  • Papaverine / pharmacology
  • Potassium / pharmacology

Substances

  • Dihydropyridines
  • Muscle Relaxants, Central
  • Gallopamil
  • Ethanol
  • 3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethyl-5-nitro-4-(2-(trifluoromethyl)phenyl)-, Methyl ester
  • Papaverine
  • Diltiazem
  • Nifedipine
  • Potassium