Chronic diazepam treatment produces regionally specific changes in GABA-stimulated chloride influx
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Biological behavior of 1, 4-benzodiazepines and 1, 4-benzothiazepines
2022, Benzodiazepine-Based Drug DiscoveryBenzodiazepine exposure induces transcriptional down-regulation of GABA<inf>A</inf> receptor α1 subunit gene via L-type voltage-gated calcium channel activation in rat cerebrocortical neurons
2020, Neuroscience LettersCitation Excerpt :In addition, a long-term in vivo treatment with flurazepam produced a reduction in the ability of zolpidem to enhance the decay constant of miniature inhibitory currents in hippocampus [42]. Finally, results from chloride uptake experiments demonstrated that both in vivo [29] and in vitro [18] treatments with benzodiazepines attenuate the ability of benzodiazepines to enhance GABA-induced 36Cl− influx. Several lines of evidence suggest a link between uncoupling and the development of tolerance.
Regulation of GABA<inf>A</inf> receptors by prolonged exposure to endogenous and exogenous ligands
2018, Neurochemistry InternationalActivation-induced regulation of GABA<inf>A</inf> receptors: Is there a link with the molecular basis of benzodiazepine tolerance?
2016, Pharmacological ResearchCitation Excerpt :Different reports have indicated that the development of tolerance after prolonged benzodiazepine administration in rodents was accompanied by an uncoupling of the GABA/benzodiazepine site interactions. Uncoupling has been detected as a decrease in the ability of benzodiazepines to potentiate the GABA currents [72] or the GABA-induced chloride influx [73], as well as a reduction in the stimulation of benzodiazepine binding by GABA [23,46,74]. Uncoupling has been observed not only after in vivo benzodiazepine treatments [23,46,74] but also as the consequence of the in vitro exposure of neuronal cultures and cell lines expressing recombinant GABAA receptors to benzodiazepines [55,57,58,75–78].
Effect of Chronic Benzodiazepine Exposure on GABA<inf>A</inf> Receptors: Regulation of GABA/Benzodiazepine Site Interactions
2016, Neuropathology of Drug Addictions and Substance Misuse Volume 3: General Processes and Mechanisms, Prescription Medications, Caffeine and Areca, Polydrug Misuse, Emerging Addictions and Non-Drug AddictionsTolerance to the sedative and anxiolytic effects of diazepam is associated with different alterations of GABA<inf>A</inf> receptors in rat cerebral cortex
2015, NeuroscienceCitation Excerpt :Long-term administration of benzodiazepines induces uncoupling in a regionally specific manner. The results from Marley and Gallager (1989) indicate that a decrease in the sensitivity of GABA-stimulated chloride influx to flunitrazepam is observed in the cerebral cortex but not in the cerebellum of rats receiving chronic diazepam treatments. Likewise, chronic flurazepam treatment in rats produces a reduction in the ability of GABA to stimulate flunitrazepam binding in the cerebral cortex, whereas the coupling between GABA and benzodiazepine sites remains unaltered in the cerebellum, medulla, striatum, hypothalamus, midbrain, hippocampus and olfactory bulb (Tietz et al., 1989).