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. 2014 Nov 12;9(11):e111899. doi: 10.1371/journal.pone.0111899

Figure 8. CogRx sigma-2/PGRMC1-selective small molecules are functional antagonists.

Figure 8

A, B Sigma-2/PGRMC1 agonist siramesine causes dose-dependent activation of caspase 3 in primary neuronal cultures (A) and in SKOV-3 human ovarian cancer cells (B) but sigma-2/PGRMC1 antagonists RHM-1, CT0109 and CT0093 do not. C, D Sigma-2/PGRMC1 agonists siramesine, WC-26 and SV-119 cause dose-dependent cell death in primary hippocampal/cortical cultures (C) and in SKOV-3 human ovarian cancer cells (D) but sigma-2/PGRMC1 antagonists RHM-1, CT0109 and CT0093 do not, except at very high concentrations (>100 µM). (E) Treatment of cultures of hippocampal and cortical cells with 20 to 80 µM SV-119 for 24 hours induced the activation of caspase 3/7 (*p<0.05 by 2-tailed Student's t-test compared to control). Co-treatment of cultures with 40 µM CT0109 or CT0093 did not increase caspase activity and blocked the activation by the agonist SV-119.