PRE084 (138847-85-8) is an agonist of the σ receptor with selectivity for the σ1 subtype (IC50’s: σ1 = 2.2nM, σ2 = 13091nM).1 PRE-084 has demonstrated neuroprotective/restorative effects in brain injury2,3 and neurodegenerative conditions4-7.
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-κB 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