An update on GABAA receptors.

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Mehta AK, Ticku MK

An update on GABAA receptors.

Brain Res Brain Res Rev. 1999 Apr;29(2-3):196-217.

PubMed ID

10209232 [ View in PubMed

]

Abstract

Recent advances in molecular biology and complementary information derived from neuropharmacology, biochemistry and behavior have dramatically increased our understanding of various aspects of GABAA receptors. These studies have revealed that the GABAA receptor is derived from various subunits such as alpha1-alpha6, beta1-beta3, gamma1-gamma3, delta, epsilon, pi, and rho1-3. Furthermore, two additional subunits (beta4, gamma4) of GABAA receptors in chick brain, and five isoforms of the rho-subunit in the retina of white perch (Roccus americana) have been identified. Various techniques such as mutation, gene knockout and inhibition of GABAA receptor subunits by antisense oligodeoxynucleotides have been used to establish the physiological/pharmacological significance of the GABAA receptor subunits and their native receptor assemblies in vivo. Radioligand binding to the immunoprecipitated receptors, co-localization studies using immunoaffinity chromatography and immunocytochemistry techniques have been utilized to establish the composition and pharmacology of native GABAA receptor assemblies. Partial agonists of GABAA receptors are being developed as anxiolytics which have fewer and less severe side effects as compared to conventional benzodiazepines because of their lower efficacy and better selectivity for the GABAA receptor subtypes. The subunit requirement of various drugs such as anxiolytics, anticonvulsants, general anesthetics, barbiturates, ethanol and neurosteroids, which are known to elicit at least some of their pharmacological effects via the GABAA receptors, have been investigated during the last few years so as to understand their exact mechanism of action. Furthermore, the molecular determinants of clinically important drug-targets have been investigated. These aspects of GABAA receptors have been discussed in detail in this review article.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Amobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Aprobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Barbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Butabarbital	GABA(A) Receptor (Protein Group)	Protein group	Humans	Yes	Positive allosteric modulator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Butalbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Butobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Heptabarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Hexobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Metharbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Methylphenobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Pentobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Phenobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Primidone	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Quinidine barbiturate	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Quinidine barbiturate	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Secobarbital	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Talbutal	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details
Thiamylal	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Agonist	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-1	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-2	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-3	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-4	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-5	Protein	Humans	Yes	Potentiator	Details
Thiopental	Gamma-aminobutyric acid receptor subunit alpha-6	Protein	Humans	Yes	Potentiator	Details