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pk 11195 and Glioma

pk 11195 has been researched along with Glioma in 27 studies

PK-11195 : A monocarboxylic acid amide obtained by formal condensation of the carboxy group of 1-(2-chlorophenyl)isoquinoline-3-carboxylic acid with the amino group of sec-butylmethylamine

Glioma: Benign and malignant central nervous system neoplasms derived from glial cells (i.e., astrocytes, oligodendrocytes, and ependymocytes). Astrocytes may give rise to astrocytomas (ASTROCYTOMA) or glioblastoma multiforme (see GLIOBLASTOMA). Oligodendrocytes give rise to oligodendrogliomas (OLIGODENDROGLIOMA) and ependymocytes may undergo transformation to become EPENDYMOMA; CHOROID PLEXUS NEOPLASMS; or colloid cysts of the third ventricle. (From Escourolle et al., Manual of Basic Neuropathology, 2nd ed, p21)

Research Excerpts

ExcerptRelevanceReference
" In the present work, we investigated the ability of the specific PBR ligands, PK 11195 or Ro5-4864, to affect mitochondrial potential and to induce apoptotic cell death in rat C6 glioma cells."3.72Peripheral benzodiazepine receptor ligands: mitochondrial transmembrane potential depolarization and apoptosis induction in rat C6 glioma cells. ( Abbracchio, MP; Ceruti, S; Chelli, B; Costa, B; Da Pozzo, E; Gremigni, V; Lena, A; Martini, C; Rossi, L; Salvetti, A; Scatena, F; Vanacore, R, 2004)
" To elucidate the biological role of the PBD receptor on mitochondria, we examined the effect of PBDs on mitochondrial morphology in C6 and T98G glioma cells using rhodamine 123 and quantitative electron microscopy."3.68Peripheral benzodiazepine induces morphological changes and proliferation of mitochondria in glioma cells. ( Becker, DP; Black, KL; Ikezaki, K; Shiraishi, T, 1991)
"The benzodiazepines, Ro 5-4864, diazepam, clonazepam, and also PK-11195, inhibited, at micromolar concentrations, the proliferation of rat C6 glioma and mouse neuro-2A neuroblastoma cells in culture."3.67Antiproliferative action of benzodiazepines in cultured brain cells is not mediated through the peripheral-type benzodiazepine acceptor. ( Gorman, AM; O'Beirne, GB; Regan, CM; Williams, DC, 1989)
" In vivo administration of 3H-labeled PK 11195 [1-(2-chlorophenyl-N-methyl-N-(1-methylpropyl)-3-isoquinoline carboxamide] or [3H]flunitrazepam with 5 mg of clonazepam per kg to rats with intracranial C6 gliomas resulted in high levels of tritiated-drug binding to the tumor as shown by quantitative autoradiography."3.67Imaging of a glioma using peripheral benzodiazepine receptor ligands. ( Ciliax, BJ; McKeever, P; Penney, JB; Starosta-Rubinstein, S; Young, AB, 1987)
"Binding of the isoquinoline PK 11195 and of the benzodiazepines Ro5-4864 and flunitrazepam was compared in glioma cells and tissues."3.67Isoquinoline and peripheral-type benzodiazepine binding in gliomas: implications for diagnostic imaging. ( Junck, L; Mancini, WR; Olson, JM; Penney, JB; Young, AB, 1988)
"TSPO in gliomas was expressed predominantly by neoplastic cells, and its expression correlated positively with BPND in the tumors."1.42The 18-kDa mitochondrial translocator protein in human gliomas: an 11C-(R)PK11195 PET imaging and neuropathology study. ( Brodbelt, A; Coope, DJ; Du Plessis, D; Durrenberger, PF; Gerhard, A; Herholz, K; Hinz, R; Jackson, A; Janczar, K; Karabatsou, K; Roncaroli, F; Su, Z; Thompson, G; Turkheimer, FE, 2015)
"Gliomas are one of the most malignant cancers."1.35TSPO over-expression increases motility, transmigration and proliferation properties of C6 rat glioma cells. ( Chelli, B; Costa, B; Da Pozzo, E; Evangelista, M; Gremigni, V; Lena, A; Martini, C; Rainaldi, G; Rechichi, M; Rossi, L; Salvetti, A; Spinetti, F, 2008)
" These studies consisted of single-dose and steady-state dosing regimen studies, the latter to assess drug distribution in normal brain and brain tumors."1.31Targeted delivery of a peripheral benzodiazepine receptor ligand-gemcitabine conjugate to brain tumors in a xenograft model. ( Adams, AL; Gallo, JM; Guo, P; Guo, Z; Li, S; Ma, J, 2001)
"C6 glioma has a KD significantly greater than rat cortex."1.28Autoradiographic study of peripheral benzodiazepine receptors in animal brain tumor models and human gliomas. ( Diksic, M; Mitsuka, S; Takada, A; Yamamoto, YL, 1992)

Research

Studies (27)

TimeframeStudies, this research(%)All Research%
pre-19907 (25.93)18.7374
1990's10 (37.04)18.2507
2000's5 (18.52)29.6817
2010's4 (14.81)24.3611
2020's1 (3.70)2.80

Authors

AuthorsStudies
Mohler, ML1
Kang, GS1
Hong, SS1
Patil, R1
Kirichenko, OV1
Li, W1
Rakov, IM1
Geisert, EE1
Miller, DD1
Gao, ZW1
Huang, YY1
Zhang, JQ1
Rong, JY1
Qiao, GY1
Chen, N1
Yu, GD1
Luo, M1
Liu, XF1
Su, Z1
Roncaroli, F1
Durrenberger, PF1
Coope, DJ1
Karabatsou, K1
Hinz, R1
Thompson, G1
Turkheimer, FE1
Janczar, K1
Du Plessis, D1
Brodbelt, A1
Jackson, A1
Gerhard, A1
Herholz, K1
Costa, B4
Da Pozzo, E3
Cavallini, C1
Taliani, S1
Da Settimo, F1
Martini, C4
Buck, JR1
McKinley, ET1
Hight, MR1
Fu, A1
Tang, D1
Smith, RA1
Tantawy, MN1
Peterson, TE1
Colvin, D1
Ansari, MS1
Baldwin, RM1
Zhao, P1
Guleryuz, S1
Manning, HC1
Crossley, EL1
Issa, F1
Scarf, AM1
Kassiou, M1
Rendina, LM1
Chelli, B2
Lena, A2
Vanacore, R1
Rossi, L2
Salvetti, A2
Scatena, F1
Ceruti, S1
Abbracchio, MP1
Gremigni, V2
Rechichi, M1
Spinetti, F1
Evangelista, M1
Rainaldi, G1
Ikezaki, K5
Nomura, T1
Takahashi, M1
Fritz-Zieroth, B1
Inamura, T1
Fukui, M1
Miyazawa, N1
Hamel, E1
Diksic, M2
Miccoli, L1
Oudard, S1
Beurdeley-Thomas, A1
Dutrillaux, B1
Poupon, MF1
Selleri, S1
Bruni, F1
Costagli, C1
Costanzo, A1
Guerrini, G1
Ciciani, G1
Guo, P1
Ma, J1
Li, S1
Guo, Z1
Adams, AL1
Gallo, JM1
Olson, JM3
McNeel, W1
Young, AB5
Mancini, WR2
Takada, A1
Mitsuka, S1
Yamamoto, YL1
Cornu, P1
Benavides, J1
Scatton, B1
Hauw, JJ1
Philippon, J1
Shiraishi, T1
Black, KL4
Becker, DP2
Santori, EM1
Smith, ML1
Payne, BA1
Toga, AW2
Broaddus, WC1
Bennett, JP1
Gorman, AM1
O'Beirne, GB1
Regan, CM1
Williams, DC1
Gildersleeve, DL2
Lin, TY1
Wieland, DM2
Ciliax, BJ3
Ferrarese, C1
Appollonio, I1
Frigo, M1
Gaini, SM1
Piolti, R1
Frattola, L1
Van Dort, ME1
Sherman, PS1
Rosenspire, KC1
Junck, L2
Starosta-Rubinstein, S1
Penney, JB2
McKeever, P1

Other Studies

27 other studies available for pk 11195 and Glioma

ArticleYear
Discovery of antiglioma activity of biaryl 1,2,3,4-tetrahydroisoquinoline derivatives and conformationally flexible analogues.
    Journal of medicinal chemistry, 2006, Sep-21, Volume: 49, Issue:19

    Topics: Animals; Antineoplastic Agents; Astrocytes; Biphenyl Compounds; Cell Line, Tumor; Cells, Cultured; D

2006
Paeoniflorin elicits the anti-proliferative effects on glioma cell via targeting translocator protein 18 KDa.
    Journal of pharmacological sciences, 2021, Volume: 145, Issue:1

    Topics: Animals; Antineoplastic Agents, Phytogenic; Cell Line, Tumor; Cell Proliferation; Disease Models, An

2021
The 18-kDa mitochondrial translocator protein in human gliomas: an 11C-(R)PK11195 PET imaging and neuropathology study.
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2015, Volume: 56, Issue:4

    Topics: Adult; Antineoplastic Agents; Astrocytoma; Biomarkers, Tumor; Blood-Brain Barrier; Brain; Brain Neop

2015
Long Residence Time at the Neurosteroidogenic 18 kDa Translocator Protein Characterizes the Anxiolytic Ligand XBD173.
    ACS chemical neuroscience, 2016, 08-17, Volume: 7, Issue:8

    Topics: Adrenal Glands; Animals; Anti-Anxiety Agents; Antineoplastic Agents; Carrier Proteins; Cell Line, Tu

2016
Quantitative, preclinical PET of translocator protein expression in glioma using 18F-N-fluoroacetyl-N-(2,5-dimethoxybenzyl)-2-phenoxyaniline.
    Journal of nuclear medicine : official publication, Society of Nuclear Medicine, 2011, Volume: 52, Issue:1

    Topics: Acetanilides; Animals; Carrier Proteins; Cell Line, Tumor; Fluorine Radioisotopes; Glioma; Isoquinol

2011
Synthesis and cellular uptake of boron-rich pyrazolopyrimidines: exploitation of the translocator protein for the efficient delivery of boron into human glioma cells.
    Chemical communications (Cambridge, England), 2011, Nov-28, Volume: 47, Issue:44

    Topics: Antineoplastic Agents; Boron Compounds; Boron Neutron Capture Therapy; Brain Neoplasms; Cell Line, T

2011
Peripheral benzodiazepine receptor ligands: mitochondrial transmembrane potential depolarization and apoptosis induction in rat C6 glioma cells.
    Biochemical pharmacology, 2004, Jul-01, Volume: 68, Issue:1

    Topics: Animals; Antineoplastic Agents; Apoptosis; Benzodiazepinones; Caspase 3; Caspases; GABA-A Receptor A

2004
TSPO over-expression increases motility, transmigration and proliferation properties of C6 rat glioma cells.
    Biochimica et biophysica acta, 2008, Volume: 1782, Issue:2

    Topics: Animals; Antineoplastic Agents; Carrier Proteins; Cell Movement; Cell Proliferation; Drug Resistance

2008
Selective and prolonged MRI enhancement by Mn-TPPS in an experimental rat brain tumour with peripheral benzodiazepine receptors.
    Neurological research, 1994, Volume: 16, Issue:5

    Topics: Animals; Brain Neoplasms; Clonazepam; Contrast Media; Glioma; Isoquinolines; Kidney; Magnetic Resona

1994
Assessment of the peripheral benzodiazepine receptors in human gliomas by two methods.
    Journal of neuro-oncology, 1998, Volume: 38, Issue:1

    Topics: Astrocytoma; Autoradiography; Biomarkers, Tumor; Brain Neoplasms; Cell Differentiation; Glioma; Huma

1998
Effect of 1-(2-chlorophenyl)-N-methyl-N-(1-methylpropyl)-3-isoquinoline carboxamide (PK11195), a specific ligand of the peripheral benzodiazepine receptor, on the lipid fluidity of mitochondria in human glioma cells.
    Biochemical pharmacology, 1999, Aug-15, Volume: 58, Issue:4

    Topics: Antineoplastic Agents; Cell Cycle; DNA, Neoplasm; GABA-A Receptor Agonists; Glioma; Humans; Isoquino

1999
2-Arylpyrazolo[1,5-a]pyrimidin-3-yl acetamides. New potent and selective peripheral benzodiazepine receptor ligands.
    Bioorganic & medicinal chemistry, 2001, Volume: 9, Issue:10

    Topics: Acetamides; Animals; Benzodiazepinones; Binding Sites; Cerebral Cortex; Clonazepam; Flumazenil; Glio

2001
Targeted delivery of a peripheral benzodiazepine receptor ligand-gemcitabine conjugate to brain tumors in a xenograft model.
    Cancer chemotherapy and pharmacology, 2001, Volume: 48, Issue:2

    Topics: Animals; Antimetabolites, Antineoplastic; Brain Neoplasms; Deoxycytidine; Drug Delivery Systems; Gem

2001
Localization of the peripheral-type benzodiazepine binding site to mitochondria of human glioma cells.
    Journal of neuro-oncology, 1992, Volume: 13, Issue:1

    Topics: Alkaline Phosphatase; Animals; Cell Line; DNA, Neoplasm; Glioma; Humans; Isoquinolines; Mitochondria

1992
Autoradiographic study of peripheral benzodiazepine receptors in animal brain tumor models and human gliomas.
    European journal of pharmacology, 1992, Sep-01, Volume: 228, Issue:2-3

    Topics: Animals; Autoradiography; Brain; Brain Neoplasms; Glioma; Humans; Isoquinolines; Kinetics; Rats; Rat

1992
Increase in omega 3 (peripheral-type benzodiazepine) binding site densities in different types of human brain tumours. A quantitative autoradiography study.
    Acta neurochirurgica, 1992, Volume: 119, Issue:1-4

    Topics: Astrocytoma; Autoradiography; Biomarkers, Tumor; Brain; Brain Neoplasms; Cerebellar Neoplasms; Gliom

1992
Peripheral benzodiazepine induces morphological changes and proliferation of mitochondria in glioma cells.
    Journal of neuroscience research, 1991, Volume: 30, Issue:3

    Topics: Animals; Benzodiazepinones; Cell Line; Clonazepam; Culture Media, Serum-Free; Fluorescent Dyes; Glio

1991
Stimulation of cell growth and DNA synthesis by peripheral benzodiazepine.
    Cancer letters, 1990, Volume: 49, Issue:2

    Topics: Animals; Benzodiazepines; Benzodiazepinones; Cell Division; Cell Line; DNA Replication; DNA, Neoplas

1990
Three-dimensional comparison of peripheral benzodiazepine binding and histological findings in rat brain tumor.
    Neurosurgery, 1990, Volume: 27, Issue:1

    Topics: Animals; Brain Neoplasms; Female; Flunitrazepam; Glioma; Isoquinolines; Rats; Rats, Inbred Strains;

1990
Peripheral-type benzodiazepine receptors in human glioblastomas: pharmacologic characterization and photoaffinity labeling of ligand recognition site.
    Brain research, 1990, Jun-04, Volume: 518, Issue:1-2

    Topics: Affinity Labels; Benzodiazepinones; Binding, Competitive; Brain Neoplasms; Cerebral Cortex; Glioma;

1990
Imaging of brain tumors using peripheral benzodiazepine receptor ligands.
    Journal of neurosurgery, 1989, Volume: 71, Issue:1

    Topics: Animals; Autoradiography; Brain Neoplasms; Clonazepam; Female; Flunitrazepam; Glioma; Image Processi

1989
Antiproliferative action of benzodiazepines in cultured brain cells is not mediated through the peripheral-type benzodiazepine acceptor.
    Journal of neurochemistry, 1989, Volume: 53, Issue:3

    Topics: Animals; Benzodiazepines; Benzodiazepinones; Blood; Cell Division; Clonazepam; Diazepam; DNA; Glioma

1989
Synthesis of a high specific activity 125I-labeled analog of PK 11195, potential agent for SPECT imaging of the peripheral benzodiazepine binding site.
    International journal of radiation applications and instrumentation. Part B, Nuclear medicine and biology, 1989, Volume: 16, Issue:4

    Topics: Animals; Brain Neoplasms; Chromatography, High Pressure Liquid; Glioma; Humans; In Vitro Techniques;

1989
Benzodiazepine receptors and diazepam-binding inhibitor in human cerebral tumors.
    Annals of neurology, 1989, Volume: 26, Issue:4

    Topics: Adolescent; Adult; Aged; Astrocytoma; Brain; Brain Neoplasms; Diazepam Binding Inhibitor; Female; Fl

1989
Radioiodinated benzodiazepines: agents for mapping glial tumors.
    Journal of medicinal chemistry, 1988, Volume: 31, Issue:11

    Topics: Animals; Autoradiography; Benzodiazepinones; Binding, Competitive; Glioma; Iodine Radioisotopes; Iso

1988
Imaging of a glioma using peripheral benzodiazepine receptor ligands.
    Proceedings of the National Academy of Sciences of the United States of America, 1987, Volume: 84, Issue:3

    Topics: Adrenal Gland Neoplasms; Animals; Flunitrazepam; Glioma; Humans; Isoquinolines; Kidney; Mice; Mice,

1987
Isoquinoline and peripheral-type benzodiazepine binding in gliomas: implications for diagnostic imaging.
    Cancer research, 1988, Oct-15, Volume: 48, Issue:20

    Topics: Benzodiazepines; Benzodiazepinones; Brain Neoplasms; Cells, Cultured; Flunitrazepam; Glioma; Humans;

1988