Tiagabine Pharmacology in Profile

@article{Brodie1995TiagabinePI,
  title={Tiagabine Pharmacology in Profile},
  author={Martin J Brodie},
  journal={Epilepsia},
  year={1995},
  volume={36}
}
  • M. Brodie
  • Published 1 June 1995
  • Biology
  • Epilepsia
Summary: Tiagabine (TGB) hydrochloride, a nipecotic acid derivative linked to a lipophilic anchor, potently and specifically inhibits uptake of the inhibitory neurotransmitter γ‐aminobu‐tyric acid (GABA) into astrocytes and neurons. With microdial‐ysis, TGB has been shown to increase extracellular overflow of GABA in the midbrain of awake rats. TGB administration prolongs neuronal depolarization induced by iontophoretically applied GABA in hippocampal slices. TGB is effective in a wide range of… 

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  • M. Benedetti
  • Biology, Medicine
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...

References

SHOWING 1-10 OF 24 REFERENCES

Pharmacokinetics of Tiagabine, a γ‐Aminobutyric Acid‐Uptake Inhibitor, in Healthy Subjects After Single and Multiple Doses

TLDR
Tiagabine (TGB) HC1, a new antiepileptic compound, is a potent and specific inhibitor of γ‐aminobutyric acid (GABA) uptake and indicated that TGB does not induce or inhibit hepaticmicrosomal enzyme systems.

The effect of two lipophilic γ‐aminobutyric acid uptake blockers in CA1 of the rat hippocampal slice

TLDR
It is found that NO–05–0328 and NO‐05‐0329, at least in vitro, are more effective than older GABA uptake inhibitors such as nipecotic acid and they therefore deserve consideration for clinical use.

Blockade of GABA Uptake with Tiagabine Inhibits Audiogenic Seizures and Reduces Neuronal Firing in the Inferior Colliculus of the Genetically Epilepsy-Prone Rat

TLDR
The blockade of GABA uptake by tiagabine may act to inhibit audiogenic seizures, in part, by intensifying these naturally occurring forms of acoustically evoked inhibition in inferior colliculus neurons.

(R)‐N‐[4,4‐Bis(3‐Methyl‐2‐Thienyl)but‐3‐en‐1‐yl]Nipecotic Acid Binds with High Affinity to the Brain γ‐Aminobutyric Acid Uptake Carrier

TLDR
It is concluded that NO 328 is a potent and selective inhibitor of neuronal and glial GABA uptake and that [3H]NO 328 are a useful radioligand for labeling the GABA uptake carrier in brain membranes.