Chemical Name: (6aR,10aR)-1-Hydroxy-3-(1-Methanesulfonylamino-4-hexyn-6-yl)-6a,7,10,10a-tetrahydro-6,6,9-trimethyl-6H-dibenzo[b,d]pyran
Biological ActivityO-2050 is an 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.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB1 receptor antagonist.
Wiley et al.
Suppression of feeding, drinking, and locomotion by a putative cannabinoid receptor 'silent antagonist.'
Gardner and Mallet
Agonists and silent antagonists in a series of cannabinoid sulfonamides.
Martin et al.
Symposium on the Cannabinoids, International Canna, 2002;
Citations for O-2050
The citations listed below are publications that use Tocris products. Selected citations for O-2050 include:
8 Citations: Showing 1 - 8
Hierarchical glucocorticoid-endocannabinoid interplay regulates the activation of the nucleus accumbens by insulin.
Authors: Pinheiro Et al.
Brain Res Bull 2016;124:222
Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
Authors: Alpár Et al.
BMC Ophthalmol 2014;5:4421
CB1 and CB2 receptors are novel molecular targets for tamox. and 4OH-Tamoxifen.
Authors: Prather Et al.
Biochem Biophys Res Commun 2013;441:339
Diacylglycerol lipase α manipulation reveals developmental roles for intercellular endocannabinoid signaling.
Authors: Keimpema Et al.
Nat Commun 2013;3:2093
CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release.
Authors: Malenczyk Et al.
J Biol Chem 2013;288:32685
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.
Authors: Brents Et al.
Biochem Pharmacol 2012;83:952
Cytochrome P450-mediated oxidative metabolism of abused synthetic cannabinoids found in K2/Spice: identification of novel cannabinoid receptor ligands.
Authors: Chimalakonda Et al.
Drug Metab Dispos 2012;40:2174
Phase I hydroxylated metabolites of the K2 synthetic cannabinoid JWH-018 retain in vitro and in vivo cannabinoid 1 receptor affinity and activity.
Authors: Brents Et al.
PLoS One 2011;6:e21917
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