Description
PRE084 (138847-85-8) is an agonist of the σ receptor with selectivity for the σ1 subtype(IC50’s: σ1 = 2.2nM, σ2 = 13091nM).1PRE-084 has demonstrated neuroprotective/restorative effects in brain injury2,3and neurodegenerative conditions4-7.
Biological Activity
High affinity, selective σ 1 agonist (K i values are 2.2 and 13091 nM for σ 1 and σ 2 receptors respectively). Selective over PCP receptors (IC 50 > 100000 nM) and several other receptor systems. Produces antiamnesic and antitussive effects in vivo .
References
[1] T P SU. Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand.[J]. Journal of Pharmacology and Experimental Therapeutics, 1991, 259 2: 543-550.
[2] E. GRIESMAIER . Neuroprotective effects of the sigma-1 receptor ligand PRE-084 against excitotoxic perinatal brain injury in newborn mice[J]. Experimental Neurology, 2012, 237 2: Pages 388-395. DOI:
10.1016/j.expneurol.2012.06.030[3] HUI DONG. Sigma-1 Receptor Modulates Neuroinflammation After Traumatic Brain Injury.[J]. Cellular and Molecular Neurobiology, 2016, 36 5: 639-645. DOI:
10.1007/s10571-015-0244-0[4] M.-S. GUZMÁN-LENIS C. C X Navarro. Selective sigma receptor agonist 2-(4-morpholinethyl)1-phenylcyclohexanecarboxylate (PRE084) promotes neuroprotection and neurite elongation through protein kinase C (PKC) signaling on motoneurons[J]. Neuroscience, 2009, 162 1: Pages 31-38. DOI:
10.1016/j.neuroscience.2009.03.067[5] A HYRSKYLUOTO. Sigma-1 receptor agonist PRE084 is protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-κB pathway[J]. Cell Death & Disease, 2013, 4 5: e646-e646. DOI:
10.1038/cddis.2013.170[6] VERONICA FRANCARDO. Pharmacological stimulation of sigma-1 receptors has neurorestorative effects in experimental parkinsonism.[J]. Brain, 2014, 137 Pt 7: 1998-2014. DOI:
10.1093/brain/awu107[7] RENZO MANCUSO . Sigma-1R Agonist Improves Motor Function and Motoneuron Survival in ALS Mice[J]. Neurotherapeutics, 2012, 9 4: Pages 814-826. DOI:
10.1007/s13311-012-0140-y
