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Relative affinities of dopaminergic drugs at dopamine D2 and D3 receptors

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Abstract

Quantitative autoradiography was used to evaluate the pharmacological profile of dopamine D2-like receptors labeled by [125I]iodosulpiride. Caudate/putamen, a brain region associated primarily with dopamine D2 receptor mRNA, was used as a prototypical D2 tissue; cerebellar lobule X (D3 mRNA associated), as a D3 tissue. 7-OH-DPAT ((±)-2-dipropylamino-7-hydroxy-1,2,3,4-tetrahydronaphthalene) exhibited selectivity for cerebellar receptors (24-fold), followed by quinpirole (6-fold). Haloperidol and domperidone were 4- and 18-fold more potent at striatal receptors, respectively. These data are in close agreement with that derived from dopamine D2 and D3 receptor-expressing cell lines.

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    In most of these regions, D2 receptors are expressed in significantly higher numbers than D3 (Gurevich and Joyce, 1999; Murray et al., 1994). There are a number of PET radiotracers in use for imaging of D2-like receptors, such as the antagonists [11C]-raclopride, [18F]-fallypride and [11C]-FLB457, and the agonist [11C]-NPA, each of which have similar affinity for D2 and D3 receptors (Halldin et al., 1995; Levant et al., 1995; Mukherjee et al., 1999). This lack of selectivity, combined with the generally higher concentration of D2 versus D3 receptors, means that specific PET signals measured with these radiotracers tend to be dominated by their D2 receptor component.

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Current affiliation: Neurocrine Biosciences. Inc., La Jolla. CA, USA.

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