PRE-084 hydrochloride | Tocris Bioscience 0589 product information

product summary

company name :

Tocris Bioscience

product type :

chemical

product name :

PRE-084 hydrochloride

catalog :

0589

quantity :

10 mg (also 50 mg)

price :

162 USD

more info or order :

Tocris Bioscience product webpage

citations: 19

Reference
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
RodrÃguez MuÃ±oz M, CortÃ©s Montero E, Pozo RodrigÃ¡lvarez A, SÃ¡nchez BlÃ¡zquez P, GarzÃ³n NiÃ±o J. The ON:OFF switch, Ïƒ1R-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 (Ïƒ1) 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
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

brand :

Tocris

master code :

0589

SKU :

0589/10

product name :

PRE-084 hydrochloride

description :

Highly selective 1 agonist

target :

Sigma1 Receptor Agonists

category :

Small Molecules

unit size :

10 mg (also 50 mg)

purity :

99%

observed molecular weight :

353.89

url print :

?utm_source=distributor&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules

details of functionality :

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.

catalog number base :

589

product keywords :

selective 1 sigma1 agonists Receptors cytoprotective Sigma1 Receptors 0589,

extended description :

Highly selective 1 agonist

chemical name text :

2-(4-Morpholinethyl) 1-phenylcyclohexanecarboxylate hydrochloride

formula :

C 19 H 27 NO 3 .HCl

formula text :

C19H27NO3.HCl

cas num :

138847-85-5

2020 USD :

155

2021 USD :

162 USD

storage :

Store at RT

more info or order :

Tocris Bioscience product webpage