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Marazziti, D. et al.

Donatella Marazziti, Stefano Baroni, Irene Masala, Gino Giannaccini, Laura Betti, Lionella Palego, Mario Catena Dell'Osso, Giorgio Consoli, Maura Castagna, Antonio Lucacchini,

[(3)H]-YM-09151-2 binding sites in human brain postmortem.

The controversial and limited data on the distribution of dopamine (DA) receptors of type 4 (D(4)) in the human brain prompted us to explore their density and pharmacological characteristics in the prefrontal cortex, striatum and hippocampus, through a series of binding assays. Brain samples were taken during autopsy from seven subjects. Tissue homogenates were incubated with increasing concentration of [(3)H]-YM-09151-2, a D(2)-like receptor antagonist, and L-745,870 and/or sulpiride to define the non-specific binding, while PPAP was used to block sigma receptors. The results showed a low density of D(4) receptors in the hippocampus only, with a preponderance of D(2)/D(3) and sigma receptors in the prefrontal cortex and striatum. In conclusion, these findings underline that it is possible to label D(4) receptors by means of [(3)H]-YM-09151-2, provided that D(2), D(3) and sigma receptors are blocked.[1]

References

[(3)H]-YM-09151-2 binding sites in human brain postmortem. Marazziti, D., Baroni, S., Masala, I., Giannaccini, G., Betti, L., Palego, L., Catena Dell'Osso, M., Consoli, G., Castagna, M., Lucacchini, A. Neurochem. Int. (2009) [Pubmed]

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