The GABAA receptor gene family: new opportunities for drug development.

Article Details

Citation

Whiting PJ

The GABAA receptor gene family: new opportunities for drug development.

Curr Opin Drug Discov Devel. 2003 Sep;6(5):648-57.

PubMed ID
14579514 [ View in PubMed
]
Abstract

gamma-Aminobutyric acid (GABA), which is the main inhibitory neurotransmitter in the mammalian brain, exerts its effects through the activation of a ligand-gated ion channel, the GABAA receptor, leading to the inhibition of the activity of neurons. A family of GABAA receptors has been identified, some of which are targets for therapeutic agents such as benzodiazepines, barbiturates and general anesthetics. Recently, novel transgenic approaches have been used to understand the function of receptor subtypes and, thereby, their therapeutic utility. Additionally, progress has been made in the development of novel receptor subtype-selective compounds. In this review, we will primarily focus on progress achieved in the understanding of the function of this receptor family, and potential exploitation for drug development.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
AmobarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
AprobarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
BarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
ButalbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
ButobarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedioneGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
HeptabarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
HexobarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
MetharbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
MethylphenobarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
PentobarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
PhenobarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
PrimidoneGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
Quinidine barbiturateGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
SecobarbitalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
TalbutalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details
ThiamylalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Agonist
Details
ThiopentalGamma-aminobutyric acid receptor subunit alpha-1ProteinHumans
Yes
Potentiator
Details