Up-regulation of L-type high voltage-gated calcium channel subunits by sustained exposure to 1,4- and 1,5-benzodiazepines in cerebrocortical neurons

J Neurochem. 2007 Dec;103(6):2518-28. doi: 10.1111/j.1471-4159.2007.04984.x. Epub 2007 Oct 18.

Abstract

The aim of this study is to examine how sustained exposure to two 1,4-benzodiazepines (BZDs) with different action period, diazepam and brotizolam, and a 1,5-BZD, clobazam, affects L-type high voltage-gated calcium channel (HVCC) functions and its mechanisms using primary cultures of mouse cerebral cortical neurons. The sustained exposure to these three BZDs increased [(45)Ca2+] influx, which was due to the enhanced [(45)Ca2+] entry through L-type HVCCs but not through of Cav2.1 and Cav2.2. Increase in [(3)H]diltiazem binding after the exposure to these three BZDs was due to the increase in the binding sites of [(3)H]diltiazem. Western blot analysis showed increase of Cav1.2 and Cav1.3 in association with the increased expression of alpha2/delta1 subunit. Similar changes in [(3)H]diltiazem binding and L-type HVCC subunit expression were found in the cerebral cortex from mouse with BZD physical dependence. These results indicate that BZDs examined here have the potential to increase L-type HVCC functions mediated via the enhanced expression of not only Cav1.2 and Cav1.3 but also alpha2/delta1 subunit after their sustained exposure, which may participate in the development of physical dependence by these BZDs.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Azepines / pharmacology
  • Benzodiazepines / pharmacology*
  • Binding, Competitive / drug effects
  • Binding, Competitive / physiology
  • Calcium Channels / drug effects
  • Calcium Channels / metabolism*
  • Calcium Channels, L-Type / drug effects
  • Calcium Channels, L-Type / metabolism*
  • Calcium Signaling / drug effects
  • Calcium Signaling / physiology
  • Cells, Cultured
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism*
  • Diazepam / pharmacology
  • Hypnotics and Sedatives / pharmacology
  • Mice
  • Neurons / drug effects
  • Neurons / metabolism*
  • Protein Subunits / drug effects
  • Protein Subunits / metabolism
  • Substance Withdrawal Syndrome / metabolism
  • Substance Withdrawal Syndrome / physiopathology
  • Up-Regulation / drug effects
  • Up-Regulation / physiology

Substances

  • Azepines
  • CACNA1C protein, mouse
  • CACNA2D1 protein, mouse
  • Cacna1d protein, mouse
  • Calcium Channels
  • Calcium Channels, L-Type
  • Hypnotics and Sedatives
  • Protein Subunits
  • Benzodiazepines
  • brotizolam
  • Diazepam