Cannabinoids modulate voltage sensitive potassium A-current in hippocampal neurons via a cAMP-dependent process

J Pharmacol Exp Ther. 1995 May;273(2):734-43.

Abstract

Previous studies have shown that cannabinoid receptor analogs increase voltage-dependent potassium A-current (IA) in cultured hippocampal cells. Because cannabinoid receptors inhibit adenylate cyclase, the present study explored whether cAMP played a role in mediating this effect on IA. The specific issue of whether cannabinoid receptor modulation of voltage-dependent IA acts via a cAMP-dependent process was investigated. The cAMP analog, 8-bromo-cAMP, as well as the adenylate cyclase stimulant forskolin, produced concentration-dependent shifts in IA that were opposite those produced by cannabinoid receptor ligands. Moreover, the phosphodiesterase inhibitor 3-isobutyl-1-methylxanthine also produced a marked negative shift in the steady-state voltage dependence of IA and increased the effect of forskolin on IA. As shown in previous studies, the cannabinoid agonist WIN 55,212-2 increased IA via a decrease in steady-state voltage-dependent inactivation of IA. WIN 55,212-2 also reversed the effects of forskolin on IA. The electrophysiological studies were paralleled by direct assays of cAMP in these cells, where cannabinoids inhibited forskolin-stimulated cAMP by 50% in a pertussis toxin-sensitive manner. The results confirmed that pertussis toxin-sensitive cannabinoid receptor-mediated changes in IA were probably the result of inhibition of adenylate cyclase. The findings are discussed in terms of modulation of IA conductance properties via cannabinoid receptor-mediated inhibition of cAMP levels within the cell.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • 1-Methyl-3-isobutylxanthine / pharmacology
  • 8-Bromo Cyclic Adenosine Monophosphate / pharmacology
  • Adenylyl Cyclases / metabolism
  • Animals
  • Benzoxazines
  • Cannabinoids / pharmacology*
  • Cells, Cultured
  • Colforsin / pharmacology
  • Cyclic AMP / physiology*
  • Enzyme Activation
  • Hippocampus / cytology
  • Hippocampus / drug effects*
  • Hippocampus / physiology
  • In Vitro Techniques
  • Ion Channel Gating
  • Morpholines / pharmacology
  • Naphthalenes / pharmacology
  • Neurons / drug effects*
  • Neurons / physiology
  • Potassium Channels / drug effects*
  • Rats
  • Receptors, Cannabinoid
  • Receptors, Drug / agonists

Substances

  • Benzoxazines
  • Cannabinoids
  • Morpholines
  • Naphthalenes
  • Potassium Channels
  • Receptors, Cannabinoid
  • Receptors, Drug
  • Colforsin
  • 8-Bromo Cyclic Adenosine Monophosphate
  • (3R)-((2,3-dihydro-5-methyl-3-((4-morpholinyl)methyl)pyrrolo-(1,2,3-de)-1,4-benzoxazin-6-yl)(1-naphthalenyl))methanone
  • Cyclic AMP
  • Adenylyl Cyclases
  • 1-Methyl-3-isobutylxanthine