PeptideDB

PRE-084 hydrochloride

CAS: 75136-54-8 F: C19H28ClNO3 W: 353.88

PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exh
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Bioactivity PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway[1][2][3][4].
Invitro PRE-084 hydrochloride (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:
In Vivo PRE-084 hydrochloride (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 hydrochloride (1 mg/kg; i.p.; single) protects the heart by activating the Akt‑eNOS pathway in myocardial infarction model[3]. Animal Model:
Name PRE-084 hydrochloride
CAS 75136-54-8
Formula C19H28ClNO3
Molar Mass 353.88
Appearance Solid
Transport Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Reference [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.