Zolpidem functionally discriminates subtypes of native GABAA receptors in acutely dissociated rat striatal and cerebellar neurons

Neuropharmacology. 1996 Feb;35(2):137-45. doi: 10.1016/0028-3908(95)00158-1.

Abstract

The whole-cell patch-clamp technique was used to compare the properties of native GABAA receptors in Purkinje and striatal neurons acutely dissociated from neonatal rat brains (7-11 days old). In symmetrical chloride concentrations and at a negative holding voltage, GABA induced inward currents in a concentration-dependent manner with EC50 values of 4 and 8 uM in Purkinje and striatal neurons, respectively. Diazepam potentiated the current induced by 1 uM GABA in Purkinje and striatal neurons with EC50 values of 28 and 42 nM and maximal potentiations of 128 and 182%, respectively. Zolpidem potentiated this GABA-induced current in Purkinje and striatal neurons with EC50 values of 33 and 195 nM and maximal potentiations of 189 and 236%, respectively. These results show that zolpidem, in contrast to diazepam, functionally discriminates subtypes of native GABAA receptors. Zolpidem has greater affinity for GABAA receptors containing omega 1 (Purkinje cells) than for those with omega 2 (striatum) sites and has higher intrinsic activity at these receptors than diazepam. These properties of zolpidem may contribute to its hypnoselective profile.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Corpus Striatum / drug effects*
  • Corpus Striatum / physiology
  • Diazepam / pharmacology
  • Dose-Response Relationship, Drug
  • Hypnotics and Sedatives / pharmacology*
  • Neurons / drug effects*
  • Neurons / physiology
  • Patch-Clamp Techniques
  • Purkinje Cells / drug effects*
  • Purkinje Cells / physiology
  • Pyridines / pharmacology*
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, GABA-A / drug effects*
  • Receptors, GABA-A / physiology
  • Zolpidem
  • gamma-Aminobutyric Acid / pharmacology

Substances

  • Hypnotics and Sedatives
  • Pyridines
  • Receptors, GABA-A
  • gamma-Aminobutyric Acid
  • Zolpidem
  • Diazepam