Gamma-aminobutyric acid benzodiazepine binding

Miller LG, Greenblatt DJ, Roy RB, et al Chronic benzodiazepine administration, II discontinuation syndrome is associated with upregulation of gamma-aminobutyric acid receptor complex binding and function. J Pharmacol Exp Ther 246 177-182, 1988b... 

Pharmacology Eszopiclone is a nonbenzodiazepine hypnotic. The precise mechanism of action of eszopiclone as a hypnotic is unknown, but its effect is believed to result from its interaction with gamma-aminobutyric acid (GABA)-receptor complexes at binding domains located close to or allosterically coupled to benzodiazepine receptors. 

Mechanism of Action A benzodiazepine that depresses all levels of the CNS, includ-ing limbic and reticular formation, by binding to benzodiazepine receptor sites on the gamma-aminobutyric acid (GABA) receptor complex. Modulates GABA, a major inhibitory neurotransmitter in the brain. Therapeutic Effect Produces anxiolytic effect,... 

Mechanism of Action A benzodiazepine that potentiates the effects of gamma-aminobutyric acid and other inhibitory neurotransmitters by binding to specific receptors in the CNS. Therapeutic Effect Produces sedative effect and skeletal muscle relaxation. 

An interaction between G. biloba administered as 80 mg leaf extract twice a day and low-dose trazodone (20 mg twice daily) was suspected in a patient with Alzheimer s disease, who took the two products together. It is postulated that a pharmacodynamic (increased gamma-aminobutyric acid-ergic activity) and pharmacokinetic mechanisms [increased metabolism of trazodone to w-chlorophenylpiperazine (w -CPP), which acts on the benzodiazepine-binding sites and releases gamma-aminobutyric acid] contribute to the observed effect (32). Table 2 provides a list of reported pharmacodynamic and pharmacokinetic interactions involving ginkgo. 

Clayton T, et al An updated unified pharmacophore model of the benzodiazepine binding site on gamma-aminobutyric acid(a) receptors Correlation with comparative models. Curr Med Chem 2007 14 2755. [PMID 18045122]... 

Diazepam binding inhibitor (DBI) is a polypeptide with a molecular weight of 9 KD. It has been isolated from rat brain by monitoring its ability to displace diazepam from the benzodiazepine (BZD) recognition site located on the extracellular domain of the type A receptor for gamma-aminobutyric acid (GABAA receptor) and from mitochondrial BZD receptor located on the outer mitochondrial membrane. This peptide is known for multiple biological effects [109]. 

Benzodiazepines all bind to a specific binding site on the gamma-aminobutyric acid (GABA) A chloride channel. The GABA chloride channel is a multi-subunit protein complex that is found in the plasma membrane of nerve cells in various parts of the CNS. When the neurotransmitter GABA binds to the chloride channel, the channel opens, allowing the influx of chloride ions into the cell. This causes hyperpolarization of the nerve cell and diminishes its response to excitatory input. The GABAa chloride channel is considered the major inhibitory system to neurotransmission in the CNS. 

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