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Characterization of Sodium-Dependent $[^{3}$H]GBR-12935 Binding in Brain: A Radioligand for Selective Labelling of the Dopamine Transport Complex
| Content Provider | Scilit |
|---|---|
| Author | Janowsky, Aaron Berger, Paul Vocci, Frank Labarca, Rodrigo Skolnick, Phil Paul, Steven M. |
| Copyright Year | 1986 |
| Description | Journal: Journal of Neurochemistry High-affinity and saturable binding sites for the diphenyl-substituted piperazine derivative [3H]GBR-12935 have been characterized in crude synaptosomal membranes prepared from rat brain. The specific binding of [3H]GBR-12935 is sodium-dependent and is unevenly distributed among various brain regions, with the highest concentration of binding sites being found in the corpus striatum and nucleus accumbens. Sodium-dependent [3H]GBR-12935 binding in all other brain areas was 10% or less of the binding found in the striatum. The affinity of [3H]GBR-12935 for binding sites in the striatum is increased in the presence of Na+ but other cations, including K+, Ca2+, or Mg2+, inhibit specific binding. There is an excellent correlation (r = 0.96, p less than 0.01) between the potencies of a series of drugs in inhibiting [3H]GBR-12935 binding to striatal membranes and their potencies in inhibiting [3H]3,4-dihydroxyphenylethylamine ([3H]dopamine) uptake in synaptosomes. Agonists and antagonists of other neurotransmitter receptor or drug recognition sites have little or no effect on specific [3H]GBR-12935 binding to striatal membranes. In addition, prior intracerebroventricular administration of 6-hydroxydopamine results in a decrease in the number of specific [3H]GBR-12935 binding sites in the striatum. These data indicate that [3H]GBR-12935 is a selective radioligand of the presynaptic dopamine transport complex in brain. |
| Related Links | http://onlinelibrary.wiley.com/doi/10.1111/j.1471-4159.1986.tb00649.x/pdf |
| Ending Page | 1276 |
| Page Count | 5 |
| Starting Page | 1272 |
| e-ISSN | 14714159 |
| DOI | 10.1111/j.1471-4159.1986.tb00649.x |
| Journal | Journal of Neurochemistry |
| Issue Number | 4 |
| Volume Number | 46 |
| Language | English |
| Publisher | Wiley-Blackwell |
| Publisher Date | 1986-04-01 |
| Access Restriction | Open |
| Subject Keyword | Journal: Journal of Neurochemistry 4‐dihydroxyphenylethylamine (dopamine) Transport |
| Content Type | Text |
| Resource Type | Article |
