PET study of carbon-11-PK 11195 binding to peripheral type benzodiazepine sites in glioblastoma: a case report.
نویسندگان
چکیده
The utility of the peripheral type benzodiazepine site ligand 11C-PK 11195, for imaging human glioma in conjunction with Positron Emission Tomography, relies on a high specific binding of the tracer to tumoral peripheral type benzodiazepines sites. In a patient with glioblastoma, we found that 11C-PK 11195 binding was two-fold higher in the tumor than in normal gray matter and that 30% of tumoral binding could be displaced by a large excess of unlabeled drug. These findings suggest that tumoral retention of the ligand is due, in part, to specific binding.
منابع مشابه
Peripheral-type benzodiazepine receptors in the living heart characterized by positron emission tomography.
The presence of specific benzodiazepine binding sites in the hearts of dogs and human beings was demonstrated in vivo by a noninvasive method, positron emission tomography (PET). An antagonist of the peripheral-type benzodiazepine binding site, PK 11195, was labeled with carbon-11, a short-lived positron emitter. When injected at high specific activity, 11C-PK 11195 was concentrated in the myoc...
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The peripheral benzodiazepine binding site ligand PK 11195 has been 125I-labeled by direct displacement of aromatic chlorine under solid-state conditions in 50-76% radiochemical yield and greater than 94% radiochemical purity. Purification by high pressure liquid chromatography increased the specific activity of the product from an initial 15-17 Ci/mmol to a final activity of 260-910 Ci/mmol. T...
متن کاملTHERAPY AND PREVENTION RECEPTOR LOCALIZATION Peripheral-type benzodiazepine receptors in the living heart characterized by positron emission tomography
The presence of specific benzodiazepine binding sites in the hearts of dogs and human beings was demonstrated in vivo by a noninvasive method, positron emission tomography (PET). An antagonist of the peripheral-type benzodiazepine binding site, PK 1 1 195, was labeled with carbon1 1, a short-lived positron emitter. When injected at high specific activity, 1C-PK l 1195 was concentrated in the my...
متن کاملPET imaging of human gliomas with ligands for the peripheral benzodiazepine binding site.
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 br...
متن کاملPresence of peripheral-type benzodiazepine binding sites on human erythrocyte membranes.
A nanomolar affinity peripheral-type benzodiazepine binding site is described in human erythrocyte membranes. [3H]PK 11195 is displaced from this binding site by unlabeled drugs with the rank order PK 11195 greater than Ro 5-4864 greater than flunitrazepam much greater than clonazepam. Neither GABA nor a non-hydrolyzable analog of GTP have an effect on binding parameters. These data provide evi...
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عنوان ژورنال:
- Journal of nuclear medicine : official publication, Society of Nuclear Medicine
دوره 32 8 شماره
صفحات -
تاریخ انتشار 1991