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 / Product Datasheet / 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:
Malik et al (2015) The effects of σ (σ1) receptor-selective ligands on muscarinic receptor antagonist-induced cognitive deficits in mice. Int J Neuropsychopharmacol 172 2519. PMID: 25573298.
Navarro et al (2015) Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine. Br J Ophthalmol 35 6639. PMID: 25926444.
Rodríguez-Muñoz et al (2015) The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Br J Pharmacol 6 35458. PMID: 26461475.
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.
Sánchez-Blázquez et al (2014) The calcium-sensitive σ-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases. J Neurosci 17 1943. PMID: 24485144.
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.
Hiranita et al (2013) Stimulants as specific inducers of dopamine-independent σ agonist self-administration in rats. ScientificWorldJournal 347 42633. PMID: 23908387.
Iñiguez et al (2013) Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation. Front Pharmacol 4 23. PMID: 23494519.
Kim et al (2012) Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression. Biochem Biophys Res Commun 426 177. PMID: 22925888.
Cantarella et al (2007) Protective effects of the σ agonist Pre-084 in the rat retina. J Pharmacol Exp Ther 91 1382. PMID: 17522150.
Brown et al (2004) Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol 141 233. PMID: 14691051.
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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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