PRE-084 Hydrochloride

Bezeichnung:PRE-084 Hydrochloride

CAS-Nr138847-85-5

Englisch Name:PRE-084 Hydrochloride

CBNumberCB0211068

SummenformelC19H27NO3

Molgewicht317.42

MOL-Datei138847-85-5.mol

PRE-084 Hydrochloride physikalisch-chemischer Eigenschaften

Siedepunkt	446.6±40.0 °C(Predicted)
Dichte	1.103±0.06 g/cm3(Predicted)
storage temp.	Store at RT
Löslichkeit	H₂O: ≤24 mg/mL
Aggregatzustand	solid
pka	5.99±0.10(Predicted)
Farbe	White
Wasserlöslichkeit	H2O: ≤24mg/mL
Stabilität	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.
InChI	1S/C19H27NO3.ClH/c21-18(23-16-13-20-11-14-22-15-12-20)19(9-5-2-6-10-19)17-7-3-1-4-8-17;/h1,3-4,7-8H,2,5-6,9-16H2;1H
InChIKey	QUJWFJNHTBKCLU-UHFFFAOYSA-N
SMILES	Cl.O=C(OCCN1CCOCC1)C2(CCCCC2)c3ccccc3

Sicherheit

WGK Germany	3
Speicherklasse	11 - Combustible Solids

Gefahreninformationscode (GHS)

PRE-084 Hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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.
Definition
ChEBI: 1-phenyl-1-cyclohexanecarboxylic acid 2-(4-morpholinyl)ethyl ester is a member of morpholines.
Biologische Aktivität
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.
Lager
Store at RT
Einzelnachweise
[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

PRE-084 Hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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