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Dihydropyridine chirality at the chromaffin cell calcium channel

Authors
Journal
Brain Research
0006-8993
Publisher
Elsevier
Publication Date
Volume
408
Identifiers
DOI: 10.1016/0006-8993(87)90405-7
Keywords
  • Calcium Antagonist
  • Calcium Channel
  • Chirality
  • Dihydropiridine Receptor
  • Catecholamine Release
  • Adrenal Medulla

Abstract

Abstract The racemic mixture of the dihydropyridine PN200-110 (Sandoz) inhibits K + voked catecholamine release from cat adrenal glands with an IC 50 of 4.1 nM; IC 50's for (+)- and (−)-PN200-110 were 0.84 and 45.8 nM, respectively. While the (+)-enantiomer of the dihydropyridine Sandoz 202–791 potentiated secretion ( EC 50 = 100nM ), the (−)-enantiomer behaved as a potent inhibitor ( IC 50 = 10nM ). Since K +-evoked 45Ca-uptake was also potently inhibited by (+)-PN200-110, it seems that the chromaffin cell dihydropyridine receptor is associated to the voltage-dependent Ca-channel and that it exhibits an exquisite stereoselectivity.

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