PRE-084 hydrochloride

Modify Date: 2024-01-02 15:34:59

PRE-084 hydrochloride Structure
PRE-084 hydrochloride structure
Common Name PRE-084 hydrochloride
CAS Number 138847-85-5 Molecular Weight 317.42
Density 1.103g/cm3 Boiling Point 446.6ºC at 760mmHg
Molecular Formula C19H27NO3 Melting Point N/A
MSDS N/A Flash Point 223.9ºC

 Use of PRE-084 hydrochloride


PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4].

 Names

Name 2-morpholin-4-ylethyl 1-phenylcyclohexane-1-carboxylate
Synonym More Synonyms

 PRE-084 hydrochloride Biological Activity

Description PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4].
Related Catalog
In Vitro PRE-084 (0.1-100 µM; 24 h) protects cultured cortical neurons against β-amyloid toxicity (maximally neuroprotective at 10 µM) and reduces the levels of proapoptotic protein Bax at 10 µM[1]. Cell Viability Assay[1] Cell Line: Cortical cells (βAP(25-35)-induced neurotoxicity model) Concentration: 0.1-100 µM Incubation Time: 24 h Result: Reduced neuronal toxicity in a bell shaped-manner and is maximally neuroprotective at 10 µM. Western Blot Analysis[1] Cell Line: Cortical cells (βAP(25-35)-induced neurotoxicity model) Concentration: 10 µM Incubation Time: 24 h Result: Reduced the levels of proapoptotic protein Bax in cortical neurons induced by βAP(25-35).
In Vivo PRE-084 (0.25 mg/kg; i.p.; 3 times a week for 8 weeks) displays beneficial effects on motor performance (improves motor neuron survival, ameliorates paw abnormality and grip strength performance) in wobbler mice, and shows neuroprotective effects (increases the levels of BDNF in the gray matter)[2]. PRE-084 (1 mg/kg; i.p.; single) protects the heart by activating the Akt‑eNOS pathway in myocardial infarction model[3]. Animal Model: Wobbler mice (4-week-old)[2]. Dosage: 0.25 mg/kg Administration: Intraperitoneal injection; 3 times a week for 8 weeks. Result: Significantly improved ameliorated paw abnormality from week 4, and notably improved paw grip strength at week 5. Reduced the number of reactive astrocytes whereas increased the number of pan-macrophage marker CD68-positive cells and CD206+ cells involved in tissue restoration. Showed 26.5% increase in the mean number of large-size NISSL-positive motor neurons. Animal Model: Adult male Sprague‑Dawley rats (220-250 g; myocardial infarction model)[3]. Dosage: 1 mg/kg Administration: Intraperitoneal injection; single. Result: Significantly decreased the degree of myocardial apoptosis. Led to significantly increased expression of p‑Akt and p‑eNOS.
References

[1]. Marrazzo A, et al. Neuroprotective effects of sigma-1 receptor agonists against beta-amyloid-induced toxicity. Neuroreport. 2005 Aug 1;16(11):1223-6.  

[2]. Peviani M, et al. Neuroprotective effects of the Sigma-1 receptor (S1R) agonist PRE-084, in a mouse model of motor neuron disease not linked to SOD1 mutation. Neurobiol Dis. 2014 Feb;62:218-32.  

[3]. Gao QJ, et al. Sigma-1 Receptor Stimulation with PRE-084 Ameliorates Myocardial Ischemia-Reperfusion Injury in Rats. Chin Med J (Engl). 2018 Mar 5;131(5):539-543.  

[4]. Su TP, et al. Sigma compounds derived from phencyclidine: identification of PRE-084, a new, selective sigma ligand. J Pharmacol Exp Ther. 1991 Nov;259(2):543-50.  

 Chemical & Physical Properties

Density 1.103g/cm3
Boiling Point 446.6ºC at 760mmHg
Molecular Formula C19H27NO3
Molecular Weight 317.42
Flash Point 223.9ºC
Exact Mass 353.175781
PSA 38.77000
LogP 3.50380
Vapour Pressure 3.61E-08mmHg at 25°C
Index of Refraction 1.532
Storage condition -20℃

 Synonyms

Tocris-0589
Pre 084
2-(4-Morpholinyl)ethyl 1-phenylcyclohexanecarboxylate hydrochloride (1:1)
1-phenyl-cyclohexanecarboxylic acid 2-morpholin-4-yl-ethyl ester
Lopac-P-2607
2-(Morpholin-4-yl)ethyl 1-phenylcyclohexanecarboxylate hydrochloride (1:1)
Cyclohexanecarboxylic acid, 1-phenyl-, 2-(4-morpholinyl)ethyl ester, hydrochloride (1:1)
PRE-084 hydrochloride