Junck L, Olson J M, Ciliax B J, Koeppe R A, Watkins G L, Jewett D M, McKeever P E, Wieland D M, Kilbourn M R, Starosta-Rubinstein S
Department of Neurology, University of Michigan, Ann Arbor.
Ann Neurol. 1989 Dec;26(6):752-8. doi: 10.1002/ana.410260611.
Human gliomas were imaged in vivo using ligands for the peripheral-type benzodiazepine binding site (or omega 3 binding site) and positron emission tomography (PET). Although gliomas have a high density of the peripheral-type benzodiazepine binding site, PET scans with a selective ligand for this site, [11C] Ro5-4864, failed to demonstrate higher radioactivity levels in human gliomas than in brain. In vitro studies of surgically removed specimens of human glioma demonstrated little binding of Ro5-4864 but high levels of binding of another selective ligand, PK 11195. Scans with [11C]PK 11195 demonstrated increased radioactivity in glioma compared to brain in 8 of 10 patients. Radioactivity in tumor and the ratios of radioactivity in tumor to that in remote gray and in white matter correlated significantly with the specific activity of [11C]PK 11195, suggesting that accumulation represents saturable high-affinity binding. We conclude that the PK 11195 manifests greater binding than Ro5-4864 to the peripheral-type benzodiazepine binding site on human gliomas and that human gliomas can be successfully imaged using [11C]PK 11195 and PET.
利用外周型苯二氮䓬结合位点（或ω3结合位点）的配体和正电子发射断层扫描（PET）对人类胶质瘤进行体内成像。尽管胶质瘤中外周型苯二氮䓬结合位点密度很高，但使用该位点的选择性配体[11C]Ro5 - 4864进行PET扫描时，并未显示出人类胶质瘤中的放射性水平高于脑内。对手术切除的人类胶质瘤标本进行的体外研究表明，Ro5 - 4864的结合很少，但另一种选择性配体PK 11195的结合水平很高。用[11C]PK 11195进行扫描显示，10例患者中有8例的胶质瘤放射性高于脑内。肿瘤中的放射性以及肿瘤与远处灰质和白质中放射性的比值与[11C]PK 11195的比活性显著相关，表明这种积聚代表可饱和的高亲和力结合。我们得出结论，PK 11195对人类胶质瘤外周型苯二氮䓬结合位点的结合比Ro5 - 4864更强，并且使用[11C]PK 11195和PET可以成功地对人类胶质瘤进行成像。
