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[3H]GBR-12935 binding to human cerebral cortex is not to dopamine uptake sites.
Umeå University, Faculty of Medicine, Department of Clinical Sciences, Psychiatry.
1994 (English)In: Journal of Neurochemistry, ISSN 0022-3042, E-ISSN 1471-4159, Vol. 62, no 1, 338-41 p.Article in journal (Refereed) Published
Abstract [en]

The binding of the dopamine uptake inhibitor [3H]GBR-12935 to 16 regions of the human brain was investigated in competition experiments with increasing concentrations of GBR-12909, mazindol, and dopamine. The methodology used included a relatively high tissue concentration (8 mg/ml) and addition of 5 mM KCl in the assay buffer. GBR-12909 inhibited 80-90% of the binding in most regions, whereas dopamine only inhibited the binding in the striatum. Mazindol inhibited only part of the cortical binding at concentrations of > 1 microM, whereas the inhibition in the caudate and the putamen also contained a high-affinity component representing the dopamine uptake site. It is concluded that the [3H]GBR-12935 binding sensitive to GBR-12909 cannot be regarded as specific binding to the dopamine uptake site because the displaceable binding most likely is not related to the dopamine uptake site.

Place, publisher, year, edition, pages
1994. Vol. 62, no 1, 338-41 p.
URN: urn:nbn:se:umu:diva-36536PubMedID: 8263533OAI: diva2:354624
Available from: 2010-10-04 Created: 2010-10-04 Last updated: 2011-05-17

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