product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
0589/10
catalog :
0589/10
quantity :
10 mg (also 50 mg)
price :
211 USD
more info or order :
citations: 22
Reference
Song L, Bekdash R, Morikawa K, Quejada J, Klein A, Aina Badejo D, et al. Sigma non-opioid receptor 1 is a potential therapeutic target for long QT syndrome. Nat Cardiovasc Res. 2022;1:142-156 pubmed publisher
Sharma N, Patel C, Shenkman M, Kessel A, Ben Tal N, Lederkremer G. The Sigma-1 receptor is an ER-localized type II membrane protein. J Biol Chem. 2021;297:101299 pubmed publisher
Cortés Montero E, Sánchez Blázquez P, Onetti Y, Merlos M, Garzón J. Ligands Exert Biased Activity to Regulate Sigma 1 Receptor Interactions With Cationic TRPA1, TRPV1, and TRPM8 Channels. Front Pharmacol. 2019;10:634 pubmed publisher
Abraham M, Fleming K, Raymond S, Wong A, Bergeron R. The sigma-1 receptor behaves as an atypical auxiliary subunit to modulate the functional characteristics of Kv1.2 channels expressed in HEK293 cells. Physiol Rep. 2019;7:e14147 pubmed publisher
Brailoiu E, Chakraborty S, Brailoiu G, Zhao P, Barr J, Ilies M, et al. Choline Is an Intracellular Messenger Linking Extracellular Stimuli to IP3-Evoked Ca2+ Signals through Sigma-1 Receptors. Cell Rep. 2019;26:330-337.e4 pubmed publisher
Atzmon A, Herrero M, Sharet Eshed R, Gilad Y, Senderowitz H, Elroy Stein O. Drug Screening Identifies Sigma-1-Receptor as a Target for the Therapy of VWM Leukodystrophy. Front Mol Neurosci. 2018;11:336 pubmed publisher
Rodríguez Muñoz M, Onetti Y, Cortés Montero E, Garzón J, Sánchez Blázquez P. Cannabidiol enhances morphine antinociception, diminishes NMDA-mediated seizures and reduces stroke damage via the sigma 1 receptor. Mol Brain. 2018;11:51 pubmed publisher
Sánchez Blázquez P, Cortés Montero E, Rodríguez Muñoz M, Garzón J. Sigma 1 Receptor Antagonists Inhibit Manic-Like Behaviors in Two Congenital Strains of Mice. Int J Neuropsychopharmacol. 2018;21:938-948 pubmed publisher
Sánchez Blázquez P, Pozo Rodrigálvarez A, Merlos M, Garzón J. The Sigma-1 Receptor Antagonist, S1RA, Reduces Stroke Damage, Ameliorates Post-Stroke Neurological Deficits and Suppresses the Overexpression of MMP-9. Mol Neurobiol. 2018;55:4940-4951 pubmed publisher
Rodríguez Muñoz M, Cortés Montero E, Pozo Rodrigálvarez A, Sánchez Blázquez P, Garzón Niño J. The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Oncotarget. 2015;6:35458-77 pubmed publisher
Navarro G, Quiroz C, Moreno Delgado D, Sierakowiak A, McDowell K, Moreno E, et al. Orexin-corticotropin-releasing factor receptor heteromers in the ventral tegmental area as targets for cocaine. J Neurosci. 2015;35:6639-53 pubmed publisher
Malik M, Rangel Barajas C, Sumien N, Su C, Singh M, Chen Z, et al. The effects of sigma (σ1) receptor-selective ligands on muscarinic receptor antagonist-induced cognitive deficits in mice. Br J Pharmacol. 2015;172:2519-31 pubmed publisher
Szabo A, Kovacs A, Frecska E, Rajnavolgyi E. 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. 2014;9:e106533 pubmed publisher
Moreno E, Moreno Delgado D, Navarro G, Hoffmann H, Fuentes S, Rosell Vilar S, et al. Cocaine disrupts histamine H3 receptor modulation of dopamine D1 receptor signaling: ?1-D1-H3 receptor complexes as key targets for reducing cocaine's effects. J Neurosci. 2014;34:3545-58 pubmed publisher
Sánchez Blázquez P, Rodríguez Muñoz M, Herrero Labrador R, Burgueno J, Zamanillo D, Garzón J. The calcium-sensitive Sigma-1 receptor prevents cannabinoids from provoking glutamate NMDA receptor hypofunction: implications in antinociception and psychotic diseases. Int J Neuropsychopharmacol. 2014;17:1943-55 pubmed publisher
Hiranita T, Soto P, Tanda G, Kopajtic T, Katz J. Stimulants as specific inducers of dopamine-independent σ agonist self-administration in rats. J Pharmacol Exp Ther. 2013;347:20-9 pubmed publisher
Iñiguez M, Punzon C, Nieto R, Burgueno J, Vela J, Fresno M. Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation. Front Pharmacol. 2013;4:23 pubmed publisher
Kim F, Schrock J, Spino C, Marino J, Pasternak G. Inhibition of tumor cell growth by Sigma1 ligand mediated translational repression. Biochem Biophys Res Commun. 2012;426:177-82 pubmed publisher
Fox J, Sakamuru S, Huang R, Teneva N, Simmons S, Xia M, et al. High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death. Proc Natl Acad Sci U S A. 2012;109:5423-8 pubmed publisher
Roh D, Choi S, Yoon S, Kang S, Moon J, Kwon S, et al. Spinal neuronal NOS activation mediates sigma-1 receptor-induced mechanical and thermal hypersensitivity in mice: involvement of PKC-dependent GluN1 phosphorylation. Br J Pharmacol. 2011;163:1707-20 pubmed publisher
Cantarella G, Bucolo C, Di Benedetto G, Pezzino S, Lempereur L, Calvagna R, et al. Protective effects of the sigma agonist Pre-084 in the rat retina. Br J Ophthalmol. 2007;91:1382-4 pubmed
Brown C, Fezoui M, Selig W, Schwartz C, Ellis J. Antitussive activity of sigma-1 receptor agonists in the guinea-pig. Br J Pharmacol. 2004;141:233-40 pubmed
product information
master code :
589
SKU :
0589/10
product name :
PRE-084 hydrochloride
unit size :
10 mg (also 50 mg)
description :
Highly selective 1 agonist
target :
Sigma1 Receptor Agonists
category :
Small Molecules
purity :
99%
observed molecular weight :
353.89
url print :
?utm_source=labome&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
PRE-084 hydrochloride is a high affinity, selective 1 agonist (Ki values are 2.2 and 13091 nM for 1 and 2 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- B signaling.
top caption :
Highly selective 1 agonist
extended description :
Highly selective 1 agonist
chemical name text :
2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate hydrochloride
formula :
C19H27NO3.HCl
formula text :
C19H27NO3.HCl
cas num :
138847-85-5
USD :
211 USD
product details :
Highly selective 1 agonist
storage :
Store at RT
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK