The Ca++/calmodulin-dependent protein kinase II inhibitors KN62 and KN93, and their inactive analogues KN04 and KN92, inhibit nicotinic activation of tyrosine hydroxylase in bovine chromaffin cells

Biochem Biophys Res Commun. 1996 Apr 5;221(1):15-8. doi: 10.1006/bbrc.1996.0536.

Abstract

The possible role of Ca++/calmodulin-dependent protein kinase II (CAM-K-II) in the nicotinic activation of tyrosine hydroxylase in intact cultured bovine adrenal chromaffin cells has been investigated. Over the concentration range 3-30 microM, KN62, a specific CAM-K-II inhibitor, inhibited basal tyrosine hydroxylase activity and the activity stimulated by nicotine or K+ depolarisation. KN04, a structural analogue of KN62 which does not inhibit CAM-K-II, produced an identical concentration-dependent inhibition of basal and nicotine-stimulated tyrosine hydroxylase activity. Another CAM-K-II inhibitor, KN93, also inhibited nicotine and K+ stimulation of tyrosine hydroxylase activity; however, an inactive analogue of KN93, KN92, mimicked these effect. The results suggest that the inhibition of nicotine- and K+-stimulated tyrosine hydroxylase activity by KN62 and KN93 is not due to their ability to inhibit CAM-K-II.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine* / analogs & derivatives*
  • Adrenal Glands / enzymology
  • Animals
  • Benzylamines / pharmacology*
  • Calcium-Calmodulin-Dependent Protein Kinases / antagonists & inhibitors*
  • Cattle
  • Cell Line
  • Chromaffin Granules / enzymology*
  • Enzyme Activation
  • Isoquinolines / pharmacology*
  • Nicotine / pharmacology*
  • Piperazines / pharmacology*
  • Sulfonamides / pharmacology*
  • Tyrosine 3-Monooxygenase / antagonists & inhibitors
  • Tyrosine 3-Monooxygenase / metabolism*

Substances

  • Benzylamines
  • Isoquinolines
  • Piperazines
  • Sulfonamides
  • KN 93
  • KN 62
  • Nicotine
  • 1-(5-Isoquinolinesulfonyl)-2-Methylpiperazine
  • Tyrosine 3-Monooxygenase
  • Calcium-Calmodulin-Dependent Protein Kinases