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J Cereb Blood Flow Metab ; 32(1): 1-5, 2012 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-22008728

RESUMO

[(11)C]PBR28 binds the 18-kDa Translocator Protein (TSPO) and is used in positron emission tomography (PET) to detect microglial activation. However, quantitative interpretations of signal are confounded by large interindividual variability in binding affinity, which displays a trimodal distribution compatible with a codominant genetic trait. Here, we tested directly for an underlying genetic mechanism to explain this. Binding affinity of PBR28 was measured in platelets isolated from 41 human subjects and tested for association with polymorphisms in TSPO and genes encoding other proteins in the TSPO complex. Complete agreement was observed between the TSPO Ala147Thr genotype and PBR28 binding affinity phenotype (P value=3.1 × 10(-13)). The TSPO Ala147Thr polymorphism predicts PBR28 binding affinity in human platelets. As all second-generation TSPO PET radioligands tested hitherto display a trimodal distribution in binding affinity analogous to PBR28, testing for this polymorphism may allow quantitative interpretation of TSPO PET studies with these radioligands.


Assuntos
Acetamidas/metabolismo , Polimorfismo de Nucleotídeo Único , Piridinas/metabolismo , Compostos Radiofarmacêuticos/metabolismo , Receptores de GABA/genética , Receptores de GABA/metabolismo , Adulto , Substituição de Aminoácidos/genética , Ligação Competitiva/genética , Plaquetas/metabolismo , Membrana Celular/genética , Membrana Celular/metabolismo , Feminino , Estudos de Associação Genética , Humanos , Isoquinolinas/metabolismo , Masculino , Tomografia por Emissão de Pósitrons , Ligação Proteica , Ensaio Radioligante , Trítio
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