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The Astrocytic GABAA/Benzodiazepine-Like Receptor: The Joker Receptor for Benzodiazepine-Mimetic Drugs?

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Long-term use of benzodiazepines as hypnotics, anxiolytics, anticonvulsants and muscle relaxing drugs is jeopardized by adverse effects on memory, addictive properties, and development of tolerance. Major efforts have gone into developing 'benzodiazepine-like' drugs that are more selective in their therapeutic effect, have additional uses and/or lack the adverse effects of benzodiazepines. The reviewed prototype patent exemplifies such efforts. Newer drugs are thought to act selectively on one of the two neuronal benzodiazepine receptors, on the astrocytic mitochondrial benzodiazepine receptor and/or on GABAA/benzodiazepine receptor complexes displaying specific subunits. It is overlooked that astrocytes also express benzodiazepine receptors that enhance depolarization-mediated entry of Ca2+ by interacting with membrane-associated GABAA-like receptors, mediating depolarization because of a high Clconcentration within astrocytes. The resulting increase in free cytosolic Ca2+, which stimulates glycogenolysis, is inhibited not only by the 'peripheral-type' benzodiazepine antagonist PK11195 but also by the 'neuronal' antagonist flumazenil. Increasing awareness of the role(s) of astrocytic Ca2+ homeostasis and energy metabolism for CNS function suggests that activation of this receptor might contribute to both therapeutic and adverse effects of benzodiazepine-like drugs. This receptor should be kept in mind when developing and testing new drugs; in turn these drugs may help elucidating its functional role.

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Keywords: Anticonvulsant; GABA; PK 11195; anxiolytic; astrocyte; benzodiazepine; calcium channel; chloride channel; flumazenil; glycogen; hypnotic

Document Type: Research Article

Affiliations: RR 2, Box 245 (738 Dickey Lake Road), Gilmour, Ontario, K0L 1W0, Canada;

Publication date: 2006-01-01

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  • Recent Patents on CNS Drug Discovery publishes review articles on recent patents in the field of CNS drug discovery e.g. novel bioactive compounds, analogs & targets. A selection of important and recent patents on CNS drug discovery is also included in the journal. The journal is essential reading for all researchers involved in CNS drug design and discovery.
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