Methyl pyropheophorbide-a analogues:: Potential fluorescent probes for the peripheral-type benzodiazepine receptor.: Effect of central metal in photosensitizing efficacy

Methyl pyropheophorbide-a analogues:: Potential fluorescent probes for the peripheral-type benzodiazepine receptor.: Effect of central metal in photosensitizing efficacy
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DOI:
10.1021/jm050039k
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发表时间:
2005-06-02
影响因子:
7.3
通讯作者:
Pandey, RK
Pandey, RK
中科院分区:
医学1区
文献类型:
--
作者:
Chen, Y;Zheng, X;Pandey, RK

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合成了焦脱镁叶绿酸及其金属配合物,研究了它们作为非放射性外周苯二氮卓受体(PBR)结合探针和光敏剂在光动力学治疗中的应用。发现它们定位于线粒体中,并显示出与PBR的显著结合。在某些情况下,PBR结合值与17(PK 11195,1-(2-氯苯基)-N-甲基-N-(1-甲基丙基)异喹啉-3-甲酰胺)相似。然而,没有观察到17的位移能力和光敏剂的光敏功效之间的直接相关性。
Pyropheophorbides and their metal complexes were synthesized to investigate their applications as nonradioactive peripheral benzodiazepine receptor (PBR) binding probes and photosensitizers for use in photodynamic therapy. They were found to be localized in mitochondria and showed significant binding to PBR. In some cases, the PBR binding values were similar to that for 17 (PK11195, 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)isoquinoline-3-carboxamide). However, no direct correlation between 17 displacement ability and photosensitizing efficacy of photosensitizers was observed.