Abstract
A major advance in the understanding of the mechanism of action of benzodiazepines and in the understanding of anxiety was the discovery, in 1977, of benzodiazepine (BZ) receptors1, 2 (for a review3). Radioactively labelled diazepam binds to a protein in the neuronal plasma membrane and this membrane protein was shown to be embedded in the outer lipid membrane of the cell. Studies with the selective neurotoxic agent kainic acid and on the mutant “nervous” mouse (nr/nr) (in which the Purkinje cells in the cerebellum completely degenerate) located the binding protein to neurons in the central nervous system. High affinity BZ receptors are not found peripherally.
This paper was also presented at the Soc. Neuroscience Minneapolis, November 1982, and at “CNS Receptors — from Molecular Pharmacology to Behaviour”, Strassbourg, September 1982.
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Braestrup, C., Nielsen, M., Honoré, T. (1984). Benzodiazepine Receptor Ligands with Positive and Negative Efficacy. In: Cattabeni, F., Nicosia, S. (eds) Principles and Methods in Receptor Binding. NATO ASI Series, vol 72. Springer, Boston, MA. https://doi.org/10.1007/978-1-4757-1577-4_8
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