Properties of ryanodine receptors in cultured cerebellar granule neurons: effects of hexachlorocyclohexane isomers and calcium

J Neurosci Res. 1997 Jan 1;47(1):27-33. doi: 10.1002/(sici)1097-4547(19970101)47:1<27::aid-jnr3>3.0.co;2-h.

Abstract

The binding of [3H]ryanodine was determined in microsomal membrane preparations obtained from cultured cerebellar granule cells. A KD of 1 nM and a Bmax of 64 fmol/mg protein were calculated from saturation experiments. This binding was calcium dependent and maximum values were obtained at 100-300 microM Ca+2. Caffeine increased [3H]ryanodine binding only at Ca+2 concentrations lower than optimum. The binding of [3H]ryanodine was inhibited by ruthenium red, procaine and the delta-isomer of hexachlorocyclohexane (delta-HCH). Dantrolene, a ryanodine receptor antagonist in skeletal sarcoplasmic reticulum, and the pesticide gamma-HCH (lindane) had no effect on [3H]ryanodine binding. The obtained binding parameters, the Ca+2 dependence and the effects of the agents tested agree with previous reports using brain microsomal membranes, further indicating a neuronal localization of [3H]ryanodine binding sites. When the interaction between dantrolene and gamma- and delta-HCH was tested, no changes were detected on the effects of HCH isomers on [3H]ryanodine binding. Dantrolene, which inhibits Ca+2 release from sarcoplasmic reticulum and from unidentified internal Ca+2 stores in neurons, also inhibits the intracellular Ca+2 mobilization induced by gamma-HCH but only marginally that induced by delta-HCH in the same preparation of cerebellar granule cells (Rosa et al.; Toxicol Appl Pharmacol, in press). Thus, the results obtained in this work verify the presence of different intracellular sites of action for the two HCH isomers: the ryanodine Ca+2 channel for delta-HCH and an unidentified dantrolene-sensitive Ca+2 channel for the gamma-HCH isomer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anesthetics, Local / pharmacology
  • Animals
  • Binding, Competitive / physiology
  • Calcium / metabolism
  • Calcium / pharmacology*
  • Calcium Channels / metabolism*
  • Calmodulin-Binding Proteins / physiology
  • Carcinogens / chemistry
  • Carcinogens / pharmacology*
  • Cells, Cultured / chemistry
  • Cells, Cultured / drug effects
  • Central Nervous System Depressants / chemistry
  • Central Nervous System Depressants / pharmacology*
  • Cerebellum / cytology
  • Coloring Agents / pharmacology
  • Dantrolene / pharmacology
  • Hexachlorocyclohexane / chemistry
  • Hexachlorocyclohexane / pharmacology*
  • Homeostasis / drug effects
  • Isomerism
  • Microsomes / chemistry
  • Microsomes / metabolism
  • Muscle Proteins / metabolism*
  • Muscle Relaxants, Central / pharmacology
  • Neurons / chemistry*
  • Neurons / cytology
  • Neurons / drug effects
  • Procaine / pharmacology
  • Rats
  • Ruthenium Red / pharmacology
  • Ryanodine / metabolism
  • Ryanodine / pharmacology
  • Ryanodine Receptor Calcium Release Channel
  • Tritium

Substances

  • Anesthetics, Local
  • Calcium Channels
  • Calmodulin-Binding Proteins
  • Carcinogens
  • Central Nervous System Depressants
  • Coloring Agents
  • Muscle Proteins
  • Muscle Relaxants, Central
  • Ryanodine Receptor Calcium Release Channel
  • Tritium
  • Ruthenium Red
  • Ryanodine
  • delta-hexachlorocyclohexane
  • Procaine
  • Hexachlorocyclohexane
  • Dantrolene
  • Calcium