2011
DOI: 10.1124/pr.110.002717
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Enhancement of GABAergic Activity: Neuropharmacological Effects of Benzodiazepines and Therapeutic Use in Anesthesiology

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Cited by 121 publications
(90 citation statements)
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References 278 publications
(344 reference statements)
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“…Among human ligand-gated ion channels, GABA A receptors have been the most heavily targeted for drug development, yielding positive allosteric modulators, such as benzodiazepines, that are widely used as antianxiety and sedative drugs (Saari et al, 2011). In addition, many surgical procedures involve drugs such as midazolam and propofol, which are employed to enhance GABA A function (Sneyd and Rigby-Jones, 2010).…”
Section: Opportunities For Novel Drug Design For Under-targeted LImentioning
confidence: 99%
“…Among human ligand-gated ion channels, GABA A receptors have been the most heavily targeted for drug development, yielding positive allosteric modulators, such as benzodiazepines, that are widely used as antianxiety and sedative drugs (Saari et al, 2011). In addition, many surgical procedures involve drugs such as midazolam and propofol, which are employed to enhance GABA A function (Sneyd and Rigby-Jones, 2010).…”
Section: Opportunities For Novel Drug Design For Under-targeted LImentioning
confidence: 99%
“…Currently, allosteric modulation of GABA A ligand-gated ion channels is a well-exploited mechanism for general anesthetics, benzodiazepine pre-anesthetic medications, and anxiolytics [65][66][67]. Agonist potentiation is also being explored to mitigate the side effects of poorly tolerated but otherwise effective analgesics acting on, for example, GABA B receptors [68] and nicotinic acetylcholine receptors [69].…”
Section: Discussionmentioning
confidence: 99%
“…The basic pharmacodynamics is by modulation of the gamma-amino-butyric acid (GABA) effect, which is the dominating inhibitory neurotransmitter in the CNS. The benzodiazepines bind to GABA receptors in the CNS thereby suppressing activity in the nerve cells (Saari et al 2011). Their high lipophilicity allows quick passage across the blood-brain barrier to produce rapid onset of action.…”
Section: Benzodiazepinesmentioning
confidence: 99%