Receptors for the age of anxiety: pharmacology of the benzodiazepines.

doi:10.1126/SCIENCE.6101294

Paper

Receptors for the age of anxiety: pharmacology of the benzodiazepines.

Published Jan 18, 1980 · J. Tallman, S. Paul, P. Skolnick

Science

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794

Citations

8

Influential Citations

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Abstract

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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Study Snapshot

Benzodiazepines effectively treat anxiety, seizures, muscle relaxation, and sedation by interacting with a high-affinity binding site in the brain, which may also interact with endogenous substances like purines and nicotinamide.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Paper

Receptors for the age of anxiety: pharmacology of the benzodiazepines.

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References

Correlation between benzodiazepine receptor occupation and anticonvulsant effects of diazepam

Diazepam's anticonvulsant effects are correlated with its occupancy of benzodiazepine receptors, suggesting that only a small fraction of these receptors are needed for complete anticonvulsant effects.

Inosine may be an endogenous ligand for benzodiazepine receptors on cultured spinal neurons.

Inosine and flurazepam both activate different conductances on spinal neurons, with flurazepam enhancing one and blocking the other.

Solubilization of benzodiazepine binding site from rat cortex.

The high-affinity benzodiazepine binding site for [3H] diazepam can be solubilized from rat brain, with binding to a single class of sites and temperature-dependent binding.

Partial agonists for brain GABA/benzodiazepine receptor complex

GABA-mimetic compounds 3-aminopropane-sulphonic acid (APS) and isoguvacine (IAA) are partial agonists for brain GABA/benzodiazepine receptor complex, while piperidine-4-sulphonic acid (PSA) and 4,5,6,7

Solubilization of gamma-aminobutyric acid receptor protein from mammalian brain.

Solubilization of gamma-aminobutyric acid receptor protein from mammalian brain reveals a major peak of binding activity with an apparent molecular weight of 9,000,000.

Some properties of brain specific benzodiazepine receptors: New evidence for multiple receptors

New evidence suggests the existence of two or more distinct types of benzodiazepine receptors, with different thermostabilities and potential for discrimination between them.

Irazepine, a noncompetitive, irreversible inhibitor of 3H-diazepam binding to benzodiazepine receptors

Irazepine is a novel benzodiazepine that acts as a noncompetitive, irreversible inhibitor of 3H-diazepam binding to benzodiazepine receptors, potentially aiding in the study of these receptors.

Is stimulation of benzodiazepine receptor binding mediated by a novel GABA receptor?

GABA stimulation of benzodiazepine receptor binding involves a novel type of GABA receptor, suggesting a novel mechanism for pharmacological effects of benzodiazepines.

Citations