The purpose of the present investigation was to compare the effects of some phenylalkylamine calcium entry blockers on postischemic energy metabolism in the isolated perfused rat brain. To differentiate between calcium entry blockade and nonspecific effects the optically active stereoisomers of emopamil were investigated. At a concentration of 10 μmol/l both gallopamil and emopamil enhanced the postischemic restoration of high-energy phosphate levels. The racemic mixture and the (–)-enan of emopamil and noremopamil caused similar metabolic changes at 1 μmol/l. The (+)-enantiomer of emopamil proved to be ineffective at either 1 or 10 μmol/l. The effects on energy metabolism were accompanied by an increase in the postischemic perfusion rate. The results suggest that the drug efficacy necessary to accelerate the restitution of postischemic energy metabolism is in the order of noremopamil > emopamil > gallopamil. The effects of the phenylalkylamine calcium entry blockers on energy metabolism are discussed in relation to vasodilation due to calcium entry blockade.

Keywords:
Calcium entry blocker, Phenylalkylamines, Enantiomers, Energy metabolism, Ischemia, Isolated perfused rat brain
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© 1988 S. Karger AG, Basel
1988
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