GABAB receptor pharmacology.

Article Details

Citation

Bowery NG

GABAB receptor pharmacology.

Annu Rev Pharmacol Toxicol. 1993;33:109-47.

PubMed ID
8388192 [ View in PubMed
]
Abstract

In conclusion, GABAB receptors appear to be of major importance in synaptic processing within the brain and are present at both post- and presynaptic sites. Their activation can hyperpolarize neurones and diminish neurotransmitter release from presynaptic terminals. We already know that drugs, i.e. baclofen, that mimic this activation are therapeutically useful, although the full significance of their use both inside and outside the brain has yet to be realized. Drugs that interfere with GABAB receptor activation should also prove to be important therapeutic agents. A number of suggestions have been proposed but it will be many years before the potential effects can be consolidated or refuted in humans. Only now are brain-penetrating GABAB antagonists being discovered, due largely to the expertise of the research group at CIBA-Geigy, Basel. The emergence of such compounds makes future studies an exciting prospect. In particular, the discovery that GABAB antagonism can suppress absence seizures in rats has provided an important therapeutic target. It is now just over ten years since we first designated the term GABAB. Since then a wealth of information has been obtained, but perhaps the best is still to come.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
ArbaclofenGamma-aminobutyric acid type B receptor subunit 1ProteinHumans
Yes
Agonist
Details
ArbaclofenGamma-aminobutyric acid type B receptor subunit 2ProteinHumans
Yes
Agonist
Details
Arbaclofen PlacarbilGamma-aminobutyric acid type B receptor subunit 1ProteinHumans
Yes
Agonist
Details
Arbaclofen PlacarbilGamma-aminobutyric acid type B receptor subunit 2ProteinHumans
Yes
Agonist
Details
BaclofenGamma-aminobutyric acid type B receptor subunit 1ProteinHumans
Unknown
Agonist
Details
BaclofenGamma-aminobutyric acid type B receptor subunit 2ProteinHumans
Yes
Agonist
Details