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Description: Putative CB1 antagonist; displays mixed activity at CB receptors
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
Purity: ≥97% (HPLC)
Biological Activity for O-2050
O-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.
Licensing Information
Sold under license from VCU-IPF
Technical Data for O-2050
| M. Wt | 417.56 |
| Formula | C23H31NO4S |
| Storage | Store at -80°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 1883545-42-3 |
| PubChem ID | 16102146 |
| InChI Key | DJTGGIYZQHHLGJ-RTBURBONSA-N |
| Smiles | OC1=CC(CC#CCCCNS(=O)(C)=O)=CC3=[C@@]1[C@@H]2CC(C)=CC[C@H]2[C@@](C)(C)O3 |
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.
Product Datasheets for O-2050
References for O-2050
References are publications that support the biological activity of the product.
Gardner and Mallet (2006) Suppression of feeding, drinking, and locomotion by a putative cannabinoid receptor 'silent antagonist.' Eur.J.Pharmacol. 530 103 PMID: 16380113
Martin et al (2002) Agonists and silent antagonists in a series of cannabinoid sulfonamides. Symposium on the Cannabinoids, International Canna
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
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Keywords: O-2050, O-2050 supplier, CB1, silent, antagonists, cannabinoids, receptors, cb1r, receptor, Receptors, 1655, Tocris Bioscience
8 Citations for O-2050
Citations are publications that use Tocris products. Selected citations for O-2050 include:
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
Alpár et al (2014) Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling. BMC Ophthalmol 5 4421 PMID: 25030704
Prather et al (2013) CB1 and CB2 receptors are novel molecular targets for tamox. 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 Ins release. J Biol Chem 288 32685 PMID: 24089517
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
Pinheiro et al (2016) Hierarchical glucocorticoid-endocannabinoid interplay regulates the activation of the nucleus accumbens by insulin. Brain Res Bull 124 222 PMID: 27208730
Keimpema et al (2013) Diacylglycerol lipase α manipulation reveals developmental roles for intercellular endocannabinoid signaling. Nat Commun 3 2093 PMID: 23806960
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Literature in this Area
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