BD 1063 dihydrochloride
Cat. No. 0883
Chemical Name: 1-[2-(3,4-Dichlorophenyl)ethyl]-4-m
Biological Activityσ1 receptor antagonist, approximately 50-fold selective over σ2 sites and ≥100-fold selective over opioid, PCP, muscarinic, dopamine, α1, α2, β adrenoceptor, 5-HT1 and 5-HT2 receptors. Prevents hyperlocomotion following cocaine administration in mice.
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 Datasheet
References are publications that support the products' biological activity.
Liu et al (2005) Cocaine up-regulated fra-2 and σ-1 receptor gene and protein expression in brain regions involved in addiction and reward. J.Pharmacol.Exp.Ther. 314 770. PMID: 15879001.
McCracken et al (1999) Novel σ receptor ligands attenuate the locomotor stimulatory effects of cocaine. Eur.J.Pharmacol. 365 35. PMID: 9988120.
Matsumoto et al (1995) Characterisation of two novel σ receptor ligands: antidystonic effects in rats suggest σ receptor antagonism. Eur.J.Pharmacol. 280 301. PMID: 8566098.
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Citations are publications that use Tocris products. Selected citations for BD 1063 dihydrochloride include:
Rodríguez-Muñoz et al (2015) The ON:OFF switch, σ1R-HINT1 protein, controls GPCR-NMDA receptor cross-regulation: implications in neurological disorders. Int J Neuropsychopharmacol 6 35458. PMID: 26461475.
Nguyen et al (2014) Involvement of sigma-1 receptors in the antidepressant-like effects of dextromethorphan. PLoS One 9 e89985. PMID: 24587167.
Pan et al (2014) σ-1 receptor antagonism restores injury-induced decrease of voltage-gated Ca2+ current in sensory neurons. Oncotarget 350 290. PMID: 24891452.
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. Nat Chem Biol 17 1943. PMID: 24485144.
Smith et al (2014) A role for picomolar concentrations of pregnenolone sulfate in synaptic activity-dependent Ca2+ signaling and CREB activation. Mol Pharmacol 86 390. PMID: 25057049.
Iñiguez et al (2013) Inhibitory effects of sigma-2 receptor agonists on T lymphocyte activation. Front Pharmacol 4 23. PMID: 23494519.
Kourrich et al (2013) Dynamic interaction between sigma-1 receptor and Kv1.2 shapes neuronal and behavioral responses to cocaine. Cell 152 236. PMID: 23332758.
Zhang et al (2013) Methylphenidate enhances NMDA-receptor response in medial prefrontal cortex via sigma-1 receptor: a novel mechanism for methylphenidate action. PLoS One 7 e51910. PMID: 23284812.
Hiranita et al (2011) Decreases in cocaine self-administration with dual inhibition of the dopamine transporter and σ receptors. J Pharmacol Exp Ther 339 662. PMID: 21859929.
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