Anavex Life Sciences Corp (AVXL)

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Sequential Cytoprotective Responses to Sigma1 Ligand–Induced Endoplasmic Reticulum Stress

"Interestingly, it appears that binding affinity does not necessarily predict drug actions: ligands with similar affinities elicit distinct responses (Fig. 1). Among the ligands used here, we find that IPAG binds Sigma1 with high affinity, Kd 3 nM (Fig. 5), and we previously determined the Sigma1 binding affinity of haloperidol as Kd 4 nM (Ryan-Moro et al., 1996). PRE-084 and (+)SKF10047 bind Sigma1 with affinities (Ki values) of 2 and 40 nM, respectively (Narayanan et al., 2011). However, only IPAG and haloperidol elicit UPR and autophagy."
§AVXL