Autoradiographic study of peripheral benzodiazepine receptors in animal brain tumor models and human gliomas |
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Institution: | 1. Institut Galien Paris-Sud, Univ Paris-Sud, UMR CNRS 8612, Faculté de Pharmacie, 5 rue Jean-Baptiste Clément, F-92296 Châtenay-Malabry Cedex, France;2. Bio-organic Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Jammu 180001, India;3. Academy of Scientific and Innovative Research (AcSIR), CSIR-IIIM, Jammu Campus, Jammu 180001, India |
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Abstract: | In vitro binding of 3H]PK-11195 (1-(2-chlorophenyl)-N-methyl-(1-methylpropyl)-3-isoquinoline carboxamide) in rodent AA ascites and C6 glioma as well as in human gliomas was investigated. The Bmax (mean ± S.D.) of AA ascites tumor and C6 glioma is 1.39 ± 0.15 pmol/mg tissue and 4.50 ± 0.76 pmol/mg tissue, respectively. This Bmax is 9 and 30 times, respectively, higher than the one found in the rat cortex (0.15 ± 0.03 pmol/mg tissue). A Bmax of 1.26 ± 0.24 pmol/mg tissue and 0.64 ± 0.08 pmol/mg tissue was found in human malignant and low grade gliomas respectively. This Bmax value should be compared to 0.35 ± 0.04 pmol/mg tissue found in the normal human cortex. There are significant (P < 0.05) differences between Bmax in tumors and normal cortex. There was no significant difference in KD between the malignant and low grade gliomas. C6 glioma has a KD significantly greater than rat cortex. In some cases of human low grade gliomas, kinetic measurements suggested the presence of two affinity receptor sites. However, at this time, heterogeneity of the tissue cannot be excluded as being at least in part a source of this. |
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