Classical benzodiazepine drugs are in wide clinical use as anxiolytics, hypnotics, anticonvulsants, and muscle relaxants. They act by enhancing the γ-aminobutyric acidA (GABAA) receptor function in the central nervous system. The pharmacological relevance of the multitude of structurally diverse GABAA receptor subtypes has only recently been identified. Based on an in vivo point mutation strategy, α1-GABAA receptors were found to mediate sedation, anterograde amnesia, and part of the seizure protection, whereas α2-GABAA receptors, but not α3-receptors, mediate anxiolysis. Rational drug targeting to specific receptor subtypes has now become possible. Only restricted neuronal networks will be modulated by the new subtype-selective drugs. Promising new anxiolytics have already been developed. A new pharmacology of the benzodiazepine site is on the horizon.
|Original language||English (US)|
|Number of pages||7|
|Journal||Journal of Pharmacology and Experimental Therapeutics|
|State||Published - 2002|
ASJC Scopus subject areas
- Molecular Medicine