RGD Reference Report - Adenosine A2A receptor stimulation decreases GAT-1-mediated GABA uptake in the globus pallidus of the rat. - Rat Genome Database

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Adenosine A2A receptor stimulation decreases GAT-1-mediated GABA uptake in the globus pallidus of the rat.

Authors: Gonzalez, B  Paz, F  Floran, L  Aceves, J  Erlij, D  Floran, B 
Citation: Gonzalez B, etal., Neuropharmacology. 2006 Jul;51(1):154-9. Epub 2006 May 30.
RGD ID: 1643197
Pubmed: PMID:16730753   (View Abstract at PubMed)
DOI: DOI:10.1016/j.neuropharm.2006.03.011   (Journal Full-text)

We examined modulation of [(3)H]GABA uptake in slices of the rat globus pallidus because stimulation of adenosine A(2A) receptors increases extracellular GABA in this structure. Pharmacological analysis showed that GAT-1 is the main transporter present in these slices. Both adenosine and the A(2A) agonist CGS 21680 reduced GABA uptake. Antagonist ZM 241385 prevented these effects. Agents that increase protein kinase A activity like forskolin and 8-bromo-cAMP also inhibited GABA uptake. The inhibition of uptake produced by these substances and by CGS 21680 was prevented by the protein kinase A blocker H-89. The protein phosphatase blocker okadaic acid reduced uptake; this effect and the response to CGS 21680 were not additive. The effective concentrations of adenosine (EC(50)=15.2microM) are within the range measured in the interstitial fluid under some physiological conditions. Thus, inhibition of uptake may be important in increasing interstitial GABA during endogenous adenosine release.

Gene Ontology Annotations    Click to see Annotation Detail View

Biological Process
TermQualifierEvidenceWithReferenceNotesSourceOriginal Reference(s)
response to purine-containing compound  IMP 1643197 RGD 

Objects Annotated

Genes (Rattus norvegicus)
Slc6a1  (solute carrier family 6 member 1)


Additional Information