TY - JOUR
T1 - Binding of 3H-WIN-35,428 and 125I-RTI-121 to human platelet membranes
AU - Marazziti, Donatella
AU - Baroni, Stefano
AU - Fabbrini, Laura
AU - Italiani, Paola
AU - Catena, Mario
AU - Dell'Osso, Bernardo
AU - Betti, Laura
AU - Giannaccini, Gino
AU - Lucacchini, Antonio
AU - Cassano, Giovanni B.
PY - 2006/3
Y1 - 2006/3
N2 - The dopamine transporter (DAT) is a protein regulating dopamine concentration in the synaptic cleft through the re-uptake mechanism. The DAT is the main target of psychostimulants and seems to play a pivotal role in neuronal degeneration and different neuropsychiatric disorders involving the dopamine system. Exhaustive research, however, regarding the presence of this protein in human platelets is still inconclusive, although it is thought that it might provide a peripheral tool to serve as a mean of exploring the same structure present in the brain. Therefore, we assessed some binding assays in platelets derived from healthy human subjects by means of 3H-WIN 35,428, a compound which is considered a selective ligand for the labelling of this protein, and by means of 125I-RTI-121, another compound with high specificity for DAT. The results showed that the binding of 3H-WIN- 35,428 was too low to enable the detection of any structure; the binding of 125I-RTI-121, on the other hand, revealed the presence of two binding sites with pharmacological profiles similar to that of the serotonin transporter (SERT). In conclusions, therefore, platelets would not seem to be a useful model for exploring the DAT, given the prevalence therein of the SERT and the difficulty of labelling the DAT with the currently available ligands.
AB - The dopamine transporter (DAT) is a protein regulating dopamine concentration in the synaptic cleft through the re-uptake mechanism. The DAT is the main target of psychostimulants and seems to play a pivotal role in neuronal degeneration and different neuropsychiatric disorders involving the dopamine system. Exhaustive research, however, regarding the presence of this protein in human platelets is still inconclusive, although it is thought that it might provide a peripheral tool to serve as a mean of exploring the same structure present in the brain. Therefore, we assessed some binding assays in platelets derived from healthy human subjects by means of 3H-WIN 35,428, a compound which is considered a selective ligand for the labelling of this protein, and by means of 125I-RTI-121, another compound with high specificity for DAT. The results showed that the binding of 3H-WIN- 35,428 was too low to enable the detection of any structure; the binding of 125I-RTI-121, on the other hand, revealed the presence of two binding sites with pharmacological profiles similar to that of the serotonin transporter (SERT). In conclusions, therefore, platelets would not seem to be a useful model for exploring the DAT, given the prevalence therein of the SERT and the difficulty of labelling the DAT with the currently available ligands.
KW - I-RTI-121
KW - H-WIN 35,428
KW - Dopamine Transporter (DAT)
KW - Human platelets
KW - Serotonin Transporter (SERT)
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U2 - 10.1007/s11064-005-9028-0
DO - 10.1007/s11064-005-9028-0
M3 - Article
C2 - 16733812
AN - SCOPUS:33744788377
VL - 31
SP - 361
EP - 365
JO - Neurochemical Research
JF - Neurochemical Research
SN - 0364-3190
IS - 3
ER -