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Brain specific benzodiazepine receptors

C Braestrup, R F Squires

The British Journal of Psychiatry : the Journal of Mental Science

|September 1, 1978

Summary

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Researchers identified specific brain binding sites for benzodiazepines, correlating drug affinity with pharmacological effects. These neuronal receptors, not on glial cells, mediate benzodiazepine actions in vivo.

Area of Science:

Neuroscience
Pharmacology
Molecular Biology

Background:

Benzodiazepines are widely used drugs with significant pharmacological and clinical effects.
The precise molecular targets mediating these effects have been a subject of extensive research.

Purpose of the Study:

To characterize the binding sites for benzodiazepines in brain membranes.
To determine the localization and function of these binding sites.

Main Methods:

In vitro radioligand binding assays using 3H-diazepam and 3H-flunitrazepam.
Selective neuronal degeneration experiments in rat models.

Main Results:

A single class of specific benzodiazepine binding sites was identified in rat and human brain membranes.

Related Experiment Videos

High correlation observed between benzodiazepine affinity for 3H-diazepam binding sites and their pharmacological effects.

Benzodiazepine binding sites are localized to neurons, not glial cells.

3H-Flunitrazepam binds to the same sites as 3H-diazepam, confirming its utility as a ligand.

Conclusions:

The in vitro binding sites for 3H-diazepam and 3H-flunitrazepam represent the neuronal receptors responsible for mediating the in vivo pharmacological and clinical effects of benzodiazepines.