caa a22 4500 469116536 CHVBK 20180323133126.0 cr unu---uuuuu 170328e19920501xx s 000 0 eng 10.1007/BF00172944 doi (NATIONALLICENCE)springer-10.1007/BF00172944 Localization of the peripheral-type benzodiazepine binding site to mitochondria of human glioma cells [Elektronische Daten] [James Olson, Wakelin McNeel, Anne Young, William Mancini] Subcellular fractionation was performed on human U251 glioblastoma cultures. In all subcellular fractions, the binding of the peripheral benzodiazepine ligand, [3H]PK 11195, correlated with the specific activity of monoamine oxidase (r = 0.95, p < 0.001) and succinate dehydrogenase (r = 0.93, p < 0.001), two mitochondrial enzymes. The specific activity of plasma membrane and nuclear markers correlated poorly with the presence of PK 11195 binding sites. These data support the mitochondrion as the primary location of peripheral-type benzodiazepine binding sites (PBBS) in human glioma cells. Mitochondria-rich preparations were then assayed for [3H]Ro5-4964 binding. Six nM [3H]Ro5-4964 failed to specifically bind to human U251 mitochondria, but bound vigorously to mitochondria from rat C6 glioma. These data indicate that the low affinity of Ro5-4864 for PBBS in human glioma cells compared to those in rat is due to interspecies receptor variation rather than impaired drug transport into human cells. Kluwer Academic Publishers, 1992 peripheral benzodiazepine receptors nationallicence glioma nationallicence mitochondria nationallicence isoquinoline binding sites nationallicence Olson James Department of Pharmacology, University of Michigan, 48109, Ann Arbor, Michigan, USA aut McNeel Wakelin Medical School, University of Michigan, 48109, Ann Arbor, Michigan, USA aut Young Anne Department of Neurology, University of Michigan, 48109, Ann Arbor, Michigan, USA aut Mancini William Department of Pharmacology, University of Michigan, 48109, Ann Arbor, Michigan, USA aut Journal of Neuro-Oncology Kluwer Academic Publishers 13/1(1992-05-01), 35-42 0167-594X 13:1<35 1992 13 11060 https://doi.org/10.1007/BF00172944 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00172944 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Olson James Department of Pharmacology, University of Michigan, 48109, Ann Arbor, Michigan, USA aut NATIONALLICENCE 700 1- McNeel Wakelin Medical School, University of Michigan, 48109, Ann Arbor, Michigan, USA aut NATIONALLICENCE 700 1- Young Anne Department of Neurology, University of Michigan, 48109, Ann Arbor, Michigan, USA aut NATIONALLICENCE 700 1- Mancini William Department of Pharmacology, University of Michigan, 48109, Ann Arbor, Michigan, USA aut NATIONALLICENCE 773 0- Journal of Neuro-Oncology Kluwer Academic Publishers 13/1(1992-05-01), 35-42 0167-594X 13:1<35 1992 13 11060 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer