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Table 1 Sigma-2 binding affinity and pancreatic cancer cell line viability, following sigma-2 receptor ligand treatment (24 h)

From: Sigma-2 receptor agonist derivatives of 1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl]piperazine (PB28) induce cell death via mitochondrial superoxide production and caspase activation in pancreatic cancer

Cmpd Affinity (K i, nM) Activity (EC50, μM)
  σ2 Panc02 KP02 KCKO MIAPaCa-2 BxPC3 AsPC-1 Panc-1
PB28a 0.68 43 >100 87 51 >100 >100 >100
PB221a 18.8 37 >100 19 50 100 >100 >100
PB183b 9.24 83 97 51 49 100 >100 >100
F281c 12.6 37 49 62 29 42 98 >100
PB282d 14.1 >100 >100 90 51 >100 >100 >100
  1. aSigma-2 binding data are from Berardi, et al. 2009 [26]; bSigma-2 binding data are from Berardi, et al. 2004 [25]; cSigma-2 binding data are from Ferorelli et al., 2007 [27]; dSigma-2 binding data are from Abate, et al., 2011 [28]. Pancreas cancer cell lines were treated with escalating doses of the sigma-2 ligands PB28, PB221, PB183, F281, PB282 or DMSO vehicle for 24 h and viability relative to vehicle determined by MTT Assay