A new benzodiazepine pharmacology.

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Mohler H, Fritschy JM, Rudolph U

A new benzodiazepine pharmacology.

J Pharmacol Exp Ther. 2002 Jan;300(1):2-8.

PubMed ID

11752090 [ View in PubMed

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Abstract

Classical benzodiazepine drugs are in wide clinical use as anxiolytics, hypnotics, anticonvulsants, and muscle relaxants. They act by enhancing the gamma-aminobutyric acid(A) (GABA(A)) receptor function in the central nervous system. The pharmacological relevance of the multitude of structurally diverse GABA(A) receptor subtypes has only recently been identified. Based on an in vivo point mutation strategy, alpha(1)-GABA(A) receptors were found to mediate sedation, anterograde amnesia, and part of the seizure protection, whereas alpha(2)-GABA(A) receptors, but not alpha(3)-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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Clobazam	GABA(A) Receptor (Protein Group)	Protein group	Humans	Yes	Positive allosteric modulator	Details
Clonazepam	GABA(A) Receptor (Protein Group)	Protein group	Humans	Yes	Positive allosteric modulator	Details
Desflurane	GABA(A) Receptor (Protein Group)	Protein group	Humans	Yes	Positive allosteric modulator	Details