Journal ArticleDOI
Receptors for the age of anxiety: pharmacology of the benzodiazepines
TLDR
Evidence indicates that the benzodiazepines exert their therapeutic effects by interacting with a high-affinity binding site (receptor) in the brain and several naturally occurring compounds, including the purines and nicotinamide, are candidates for this role.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.read more
Citations
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Précis of The Neuropsychology of Anxiety: An Enquiry into the Functions of the Septo-Hippocampal System..
TL;DR: It is proposed that these drugs reduce anxiety by impairing the functioning of a widespread neural system including the septo-hippocampal system (SHS), the Papez circuit, the prefrontal cortex, and ascending monoaminergic and cholinergic pathways which innervate these forebrain structures.
Journal ArticleDOI
Steroid Hormone Metabolites are Barbiturate-Like Modulators of the GABA Receptor
Maria Dorota Majewska,Neil L. Harrison,Rochelle D. Schwartz,Jeffery L. Barker,Steven M. Paul +4 more
TL;DR: Two metabolites of the steroid hormones progesterone and deoxycorticosterone are potent barbiturate-like ligands of the gamma-aminobutyric acid (GABA) receptor-chloride ion channel complex and potentiated the inhibitory actions of GABA in cultured rat hippocampal and spinal cord neurons, which may explain the ability of certain steroid hormones to rapidly alter neuronal excitability.
The neuropsychology of anxiety
TL;DR: This paper is a rough precis of a recent book concerned with the question: what are the brain structures which mediate the psychology as well as the neurology of anxiety?
Book
The neuropsychology of anxiety
TL;DR: GRAY as mentioned in this paper discusses the brain structures which mediate the psychology as well as the neurology of anxiety in animals and proposes a kind of crutch or bridge to get across from the human domain on one side to the animal domain on the other.
Journal ArticleDOI
GABA‐Benzodiazepine‐Barbiturate Receptor Interactions
TL;DR: Evidence supports the model for a complex containing receptor sites for GABA, benzodiazepines, and picrotoxininl barbiturates, as well as the chloride ionophore, and thus the relevance of GABA to the actions of the other drugs.
References
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Journal ArticleDOI
Benzodiazepine receptor: demonstration in the central nervous system
Hanns Möhler,T Okada +1 more
TL;DR: Competition for the receptor by various benzodiazepines closely parallels their pharmacological potency, and binding to the receptor is stereospecific.
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Specific benzodiazepine receptors in rat brain characterized by high-affinity (3H)diazepam binding
TL;DR: Specific [3H]diazepam binding to membranes appears to be restricted to brain, where it is unevenly distributed: the density of diazepam receptors is about five times higher in cortex (the highest density) than in pons-meddula (lowest density).
Amino acid transmitters in the mammalian central nervous system
TL;DR: Evidence for A m i n o Acids as T ransmi t t e r s as well as evidence for Synthesis and Storage are presented.
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GABAergic modulation of benzodiazepine binding site sensitivity.
TL;DR: GA can modulate the responsiveness of this BZ binding site since the addition of GABA to cortical membranes in vitro results in an increased affinity of the 3H-diazepam binding site for its ligand.
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Opiate receptor: autoradiographic localization in rat brain.
TL;DR: Silver grains indicative of the binding of labeled [3H]diprenorphine are discretely localized in numerous areas of the brain with very high densities in the locus coeruleus, the substantia gelatinosa of the spinal cord, and in clusters within the caudate-putamen, amygdala, and parts of the periventricular gray matter.