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Central-type and peripheral-type benzodiazepine receptors.

V Saano1

  • 1Department of Pharmacology and Toxicology, University of Kuopio, Finland.

Annals of Clinical Research
|January 1, 1988
PubMed
Summary

Benzodiazepine receptors in the brain and periphery were discovered after widespread use. Research is advancing with the identification of endogenous ligands for both central and peripheral benzodiazepine receptors, promising new drug development.

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Area of Science:

  • Neuropharmacology
  • Molecular Biology

Background:

  • Benzodiazepines have been used as anxiolytics and anticonvulsants for over a decade.
  • Both central nervous system (CNS) and peripheral binding sites for benzodiazepines exist.
  • Central benzodiazepine receptors are linked to gamma-amino butyric acid (GABA) receptors in the brain.

Purpose of the Study:

  • To explore the properties and functions of central and peripheral benzodiazepine receptors.
  • To understand the mechanisms underlying benzodiazepine actions.
  • To highlight the potential for new drug development targeting these receptors.

Main Methods:

  • Pharmacological characterization of benzodiazepine binding sites.
  • Investigation of receptor coupling with other neurotransmitter systems (e.g., GABA).
  • Identification of endogenous ligands for benzodiazepine receptors.

Main Results:

  • Central benzodiazepine receptors mediate acute CNS effects like anxiety and convulsions, which can be modulated by inverse agonists and blocked by antagonists.
  • Peripheral benzodiazepine receptors appear to be involved in slower drug actions, such as cell proliferation modulation.
  • Endogenous ligands, diazepam binding inhibitor (DBI) for central receptors and porphyrins for peripheral receptors, have been identified.

Conclusions:

  • Central benzodiazepine receptors offer significant potential for developing novel therapeutic agents.
  • Further research into peripheral benzodiazepine receptor function is warranted.
  • The discovery of endogenous ligands will likely accelerate research in this field.

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