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| | [3H]PK 11195 radio-assay |
| Description: | For the assays described herein systemic injections of kainic in rats were applied and also contusion (Veenman et al. 2002; Soustiel et al. Neuropathol Appl Neurobiol. 2008; Soustiel et al. Exp Neurol. 2008). These models present very well defined cell death in the brain. Cell death in the brain is the major pathological characteristic of progressing neurodegeneration common to brain diseases. As the compounds of the present invention are designed to prevent cell death in the brain as a consequence of disease and progressing brain damage after injury, including behavioral impairments, animal models displaying cell death in the brain are the models of choice for displaying the protective capabilities of the compounds of the invention. For these reasons the R6-2 model for Huntington Disease was chosen to test the effectiveness of Compound 1 and to compare the effectiveness of Compound 1 with those of the compound of U.S. Pat. No. 8,541,428 (Cpd A) and with the classical TSPO ligand PK 11195, as well as other compounds disclosed herein. Compounds 5 and 6 were also tested in the same R6-2 model. |
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