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Science 18 January 1980:
Vol. 207. no. 4428, pp. 274 - 281
DOI: 10.1126/science.6101294
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Articles

Science, Vol 207, Issue 4428, 274-281
Copyright © 1980 by American Association for the Advancement of Science

articles

Receptors for the age of anxiety: pharmacology of the benzodiazepines

JF Tallman, SM Paul, P Skolnick, and DW Gallager

Investigation of the actions of the benzodiazepines has provided insights into the neurochemical mechanisms underlying anxiety, seizures, muscle relaxation, and sedation. Behavioral, electrophysical, pharmacological, and biochemical evidence indicates that the benzodiazepines exert their therapeutic effects by interacting with a high-affinity binding site (receptor) in the brain. The benzodiazepine receptor interacts with a receptor for gamma-aminobutyric acid, a major inhibitory neurotransmitter, and enhances its inhibitory effects. The benzodiazepine receptor may also interact with endogenous substances and several naturally occurring compounds, including the purines and nicotinamide, are candidates for this role. Both the purines and nicotinamide possess some benzodiazepine-like properties in vivo, although further work will be required to confirm their possible roles as endogenous benzodiazepines.


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