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| | PRE-084 Basic information |
| Product Name: | PRE-084 | | Synonyms: | 2-(4-MORPHOLINETHYL) 1-PHENYLCYCLOHEXANECARBOXYLATE HYDROCHLORIDE;PRE-084;PRE-084 HYDROCHLORIDE;PRE-084HCl;2-(4-morpholino)ethyl-1-phenylcyclohexane-1-carboxylate;1-Phenylcyclohexanecarboxylic acid 2-morpholinoethyl ester;4-MeO-PBP;I-AMB | | CAS: | 138847-85-5 | | MF: | C19H27NO3 | | MW: | 317.42 | | EINECS: | | | Product Categories: | Sigma receptor;pharmaceuticals | | Mol File: | 138847-85-5.mol |  |
| | PRE-084 Chemical Properties |
| Boiling point | 446.6±40.0 °C(Predicted) | | density | 1.103±0.06 g/cm3(Predicted) | | storage temp. | Store at RT | | solubility | H2O: ≤24 mg/mL | | form | solid | | pka | 5.99±0.10(Predicted) | | color | White | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or distilled water may be stored at -20°C for up to 3 months. |
| | PRE-084 Usage And Synthesis |
| 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).1?PRE-084 has demonstrated neuroprotective/restorative effects in brain injury2,3?and neurodegenerative conditions4-7. | | Definition | ChEBI: 1-phenyl-1-cyclohexanecarboxylic acid 2-(4-morpholinyl)ethyl ester is a member of morpholines. | | 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 . | | Biochem/physiol Actions | PRE-084 is a potent and highly selective σ1 opioid receptor agonist. It offers neuroprotection upon embolic stroke. | | storage | Store at RT | | References | 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 |
| | PRE-084 Preparation Products And Raw materials |
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