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HomeProduct name listPRE-084

PRE-084

Synonym(s):2-(4-morpholinethyl)-1-phenylcyclohexanecarboxylate hydrochloride

PRE-084 Structural

What is PRE-084?

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.

What are the applications of Application

PRE-084 Hydrochloride is a high affinity selective σ1 agonist, antiamnesic, antitussive, and activator of NF-κB signaling.

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

Properties of PRE-084

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.

Safety information for PRE-084

Signal word Warning
Pictogram(s)
ghs
Exclamation Mark
Irritant
GHS07
GHS Hazard Statements H302:Acute toxicity,oral
Precautionary Statement Codes P280:Wear protective gloves/protective clothing/eye protection/face protection.
P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

Computed Descriptors for PRE-084

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