Novel PET ligands for brain-function imaging with the brain-targeting peptide molecules

我们研究了我们最初建立的脑靶向（BT）肽用于脑PET成像的新型配体开发的可行性。我们成功地证明了[11 C]MQNB-BT肽缀合物在脑穿透活性中的潜力，而[11 C]MQNB本身没有这种活性。定量分析表明，[11 C]MQNB-BT肽缀合物具有约10%的[11 C]NMPB的脑穿透活性，其可透过血脑屏障。这些结果表明，BT肽具有作为脑功能成像工具的DDS载体的潜力。

We investigated the feasibility of our originally established brain-targeting (BT) peptide for novel ligand development of brain PET imaging. We successfully demonstrated the potential of [11C]MQNB-BT peptide conjugate in brain-penetrating activity, whereas [11C]MQNB itself has no such activity. Quantitative analysis indicated that [11C]MQNB-BT peptide conjugate had about 10% brain-penetrating activity of [11C]NMPB, which is permeable to blood-brain barrier. These results suggested that BT peptide has a potential of a DDS carrier for brain function imaging tools.