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O-2050

1655 8 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1655/10
O-2050 | CAS No. 1883545-42-3 | Cannabinoid R1/CB1 Antagonists
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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%

Product Details
Citations (8)
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Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

Technical Data

M.Wt:
417.56
Formula:
C23H31NO4S
Solubility:
Soluble to 100 mM in ethanol and to 100 mM in DMSO
Purity:
≥97%
Storage:
Store at -80°C
CAS No:
1883545-42-3

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.

Additional Information

Licensing Caveats:
Sold under license from VCU-IPF

Background References

  1. Structural and pharmacological analysis of O-2050, a putative neutral cannabinoid CB1 receptor antagonist.
    Wiley et al.
    Eur.J.Pharmacol., 2011;651:96
  2. Suppression of feeding, drinking, and locomotion by a putative cannabinoid receptor 'silent antagonist.'
    Gardner and Mallet
    Eur.J.Pharmacol., 2006;530:103
  3. Agonists and silent antagonists in a series of cannabinoid sulfonamides.
    Martin et al.
    Symposium on the Cannabinoids, International Canna, 2002;

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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

  1. Hierarchical glucocorticoid-endocannabinoid interplay regulates the activation of the nucleus accumbens by insulin.
    Authors: Pinheiro Et al.
    Brain Res Bull  2016;124:222
  2. Endocannabinoids modulate cortical development by configuring Slit2/Robo1 signalling.
    Authors: Alpár Et al.
    BMC Ophthalmol  2014;5:4421
  3. CB1 and CB2 receptors are novel molecular targets for tamox. and 4OH-Tamoxifen.
    Authors: Prather Et al.
    Biochem Biophys Res Commun  2013;441:339
  4. Diacylglycerol lipase α manipulation reveals developmental roles for intercellular endocannabinoid signaling.
    Authors: Keimpema Et al.
    Nat Commun  2013;3:2093
  5. CB1 cannabinoid receptors couple to focal adhesion kinase to control Ins release.
    Authors: Malenczyk Et al.
    J Biol Chem  2013;288:32685
  6. 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
  7. 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
  8. 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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VersaClone cDNA Plasmids

Human Cannabinoid R1/CB1/CNR1 (NP_057167) VersaClone cDNA

RDC0109

Mouse Cannabinoid R1/CB1/CNR1 (NP_031752) VersaClone cDNA

RDC0222

Rat Cannabinoid R1/CB1/CNR1 (NP_036916) VersaClone cDNA

RDC0757

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