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(3H)tiagabine binding to GABA uptake sites in human brain.
Linköping University, Faculty of Health Sciences. Linköping University, Department of Neuroscience and Locomotion, Geriatrics. Östergötlands Läns Landsting, MC - Medicincentrum, Geriatrik-LAH.
1999 (English)In: Brain Research, ISSN 0006-8993, Vol. 18, no 1-2, 183-188 p.Article in journal (Refereed) Published
Abstract [en]

The binding of [H-3]tiagabine ((RS-1-(4,4-(3-methyl-2-thienyl)-3-butenyl)-3 carboxylic acid) to homogenates of frozen post-mortem human brain has been characterized. Inhibition experiments with gamma-aminobutyric acid (GAB,4), GABA uptake inhibitors, ligands active at postsynaptic GABA receptors and receptors for other neurotransmitters, suggest that [H-3]tiagabine binds with high affinity to GABA uptake sites. Inhibition and kinetic experiments suggests that 70%-80% of the binding is to a high affinity site. Saturation experiments showed that the binding was saturable. B-max was 3.4 pmol/mg protein and K-d 16 nM in frontal cortex. The dissociation constants (K-d) measured in kinetic and equilibrium experiments were in the same range (16-56 nM). The regional distribution was studied in nine brain regions and the binding was heterogenous, with the highest binding in frontal cortex and parietal cortex and the lowest binding in nucleus caudatus and putamen. This is, to our knowledge, the first study on [H-3]tiagabine binding in human tissue. It is concluded that [H-3]tiagabine binding can be used as a specific marker for the GABA transporter GAT-1 in homogenates of human brain.

Place, publisher, year, edition, pages
1999. Vol. 18, no 1-2, 183-188 p.
Keyword [en]
GABA, tiagabine, uptake site, GAT-1, frontal cortex, human
National Category
Medical and Health Sciences
URN: urn:nbn:se:liu:diva-27874Local ID: 12634OAI: diva2:248426
Available from: 2009-10-08 Created: 2009-10-08 Last updated: 2009-11-02

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