Biochemicals & reagents
1) Su et al. (1991), Sigma compounds derived from phencyclidine. Identification of PRE-084, a new selective sigma ligand; J.Pharmacol.Exp.Ther. 259 543 2) Griesmaier et al. (2012), Neuroprotective effects of the sigma-1 receptor ligand PRE-084 against excitotoxic perinatal brain injury in newborn mice; Exp.Neurol. 237 388 3) Dong et al. (2016), Sigma-1 Receptor Modulates Neuroinflammation After Traumatic Brain Injury; Cell Mol.Neurobiol. 36 639 4) Guzman-Lenis et al. (2009), Selective sigma receptor agonist 2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate (PRE084) promotes neuroprotection and neurite elongation through protein kinase C (PKC) signaling on motoneurons; Neuroscience 162 31 5) Hyrskyluoto et al. (2013), Sigma-1 receptor agonist PRE084 in protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-kB pathway; Cell Death Dis. 4 e646 6) Francardo et al. (2014), Pharmacological stimulation of sigma-1 receptors has neurorestorative effects in experimental parkinsonism; Brain 137(Pt7) 1998 7) Mancuso et al. (2012), Sigma-1R agonist improves motor function and motoneuron survival in ALS mice; Neurotherapeutics 9 814
PRE084 is an agonist of the σ receptor with selectivity for the σ1 subtype with IC50’s of σ1 = 2.2nM and σ2 = 13091nM (1). This compound has demonstrated neuroprotective/restorative effects in brain injury (2,3) and for neurodegenerative conditions (4-7).