GABAB receptor pharmacology.
Article Details
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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
Drug Target Kind Organism Pharmacological Action Actions Arbaclofen Gamma-aminobutyric acid type B receptor subunit 1 Protein Humans YesAgonistDetails Arbaclofen Gamma-aminobutyric acid type B receptor subunit 2 Protein Humans YesAgonistDetails Arbaclofen Placarbil Gamma-aminobutyric acid type B receptor subunit 1 Protein Humans YesAgonistDetails Arbaclofen Placarbil Gamma-aminobutyric acid type B receptor subunit 2 Protein Humans YesAgonistDetails Baclofen Gamma-aminobutyric acid type B receptor subunit 1 Protein Humans UnknownAgonistDetails Baclofen Gamma-aminobutyric acid type B receptor subunit 2 Protein Humans YesAgonistDetails