Originally defined as a high affinity cannabinoid CB1 receptor silent antagonist. Acts as a partial agonist in inhibiting forksolin-induced cyclic AMP stimulation (EC50 = 40.4 nM). Decreases food intake and stimulates locomotor activity in rodents. Antagonizes effects of CP55,940 (Cat. No. 0949) in vitro.
Sold under license from VCU-IPF
|Storage||Store at -80°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 417.56. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.39 mL||11.97 mL||23.95 mL|
|5 mM||0.48 mL||2.39 mL||4.79 mL|
|10 mM||0.24 mL||1.2 mL||2.39 mL|
|50 mM||0.05 mL||0.24 mL||0.48 mL|
References are publications that support the products' biological activity.
Gardner and Mallet (2006) Suppression of feeding, drinking, and locomotion by a putative cannabinoid receptor 'silent antagonist.' Eur.J.Pharmacol. 530 103 PMID: 16380113
Wiley et al (2011) Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB1 receptor antagonist. Eur.J.Pharmacol. 651 96 PMID: 21114999
If you know of a relevant reference for O-2050, please let us know.
Keywords: O-2050, supplier, CB1, silent, antagonists, cannabinoids, receptors, cb1r, receptor, CB1, Receptors, CB1, Receptors, Tocris Bioscience
7 Citations for O-2050
Citations are publications that use Tocris products. Selected citations for O-2050 include:
Keimpema et al (2013) Diacylglycerol lipase α manipulation reveals developmental roles for intercellular endocannabinoid signaling. Nat Commun 3 2093 PMID: 23806960
Brents et al (2012) Monohydroxylated metabolites of the K2 synthetic cannabinoid JWH-073 retain intermediate to high cannabinoid 1 receptor (CB1R) affinity and exhibit neutral antagonist to partial agonist activity. Biochem Pharmacol 83 952 PMID: 22266354
Chimalakonda et al (2012) Cytochrome P450-mediated oxidative metabolism of abused synthetic cannabinoids found in K2/Spice: identification of novel cannabinoid receptor ligands. Drug Metab Dispos 40 2174 PMID: 22904561
Alpár et al (2014) Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling. BMC Ophthalmol 5 4421 PMID: 25030704
Brents et al (2011) Phase I hydroxylated metabolites of the K2 synthetic cannabinoid JWH-018 retain in vitro and in vivo cannabinoid 1 receptor affinity and activity. PLoS One 6 e21917 PMID: 21755008
Prather et al (2013) CB1 and CB2 receptors are novel molecular targets for Tamoxifen and 4OH-Tamoxifen. Biochem Biophys Res Commun 441 339 PMID: 24148245
Malenczyk et al (2013) CB1 cannabinoid receptors couple to focal adhesion kinase to control insulin release. J Biol Chem 288 32685 PMID: 24089517
Do you know of a great paper that uses O-2050 from Tocris? If so please let us know.
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Literature in this Area
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The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.