Cat. No. 0589
Chemical Name: 2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate hydrochloride
Biological ActivityHigh affinity, selective σ1 agonist (Ki values are 2.2 and 13091 nM for σ1 and σ2 receptors respectively). Selective over PCP receptors (IC50 > 100000 nM) and several other receptor systems. Produces antiamnesic and antitussive effects in vivo. Also exhibits protective effects in PC6.3 cells expressing mutant huntingtin by activating NF-κB signaling.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Hyrskyluoto et al (2013) Sigma-1 receptor agonist PRE084 is protective against mutant huntingtin-induced cell degeneration: involvement of calpastatin and the NF-κB pathway. Cell Death Dis. 4 e646. PMID: 23703391.
Brown et al (2004) Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br.J.Pharmacol. 141 233. PMID: 14691051.
Maurice et al (1999) The attenuation of learning impairments induced after exposure to CO or trimethyltin in mice by sigma (σ) receptor ligands involves both σ1 and σ2 sites. Br.J.Pharmacol. 127 335. PMID: 10385231.
Su et al (1991) Sigma compounds derived from phencyclidine. Identification of PRE-084, a new selective sigma ligand. J.Pharmacol.Exp.Ther. 259 543. PMID: 1658302.
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Citations are publications that use Tocris products. Selected citations for PRE-084 hydrochloride include:
Moreno et al (2014) Cocaine disrupts histamine H3 receptor modulation of dopamine D1 receptor signaling: σ1-D1-H3 receptor complexes as key targets for reducing cocaine's effects. J Neurosci 34 3545. PMID: 24599455.
Szabo et al (2014) Psychedelic N,N-dimethyltryptamine and 5-methoxy-N,N-dimethyltryptamine modulate innate and adaptive inflammatory responses through the sigma-1 receptor of human monocyte-derived dendritic cells. PLoS One 9 e106533. PMID: 25171370.
Iñiguez et al (2013) Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation. Front Pharmacol 4 23. PMID: 23494519.
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Keywords: PRE-084 hydrochloride, supplier, selective, σ1, sigma1, agonists, Receptors, cytoprotective, Tocris Bioscience, σ1 Receptor Agonist products
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