Biological Activity
Potent, selective CB1 cannabinoid receptor antagonist/inverse agonist (Ki values are 12 and 4200 nM for CB1 and CB2 receptors respectively). Increases locomotor activity following systemic administration in vivo. Analog of SR141716A (Ki = 14 nM).
Licensing Information
Sold with the permission of the University of Connecticut
Technical Data
| M. Wt | 557.22 |
| Formula | C21H19Cl2IN4O2 |
| Storage | Desiccate at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 202463-68-1 |
| PubChem ID | 4302962 |
| InChI Key | AJFFBPZYXRNAIC-UHFFFAOYSA-N |
| Smiles | CC1=C(N(N=C1C(=O)NN1CCOCC1)C1=C(Cl)C=C(Cl)C=C1)C1=CC=C(I)C=C1 |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 41.79 | 75mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 557.22. 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 | 1.79 mL | 8.97 mL | 17.95 mL |
| 5 mM | 0.36 mL | 1.79 mL | 3.59 mL |
| 10 mM | 0.18 mL | 0.9 mL | 1.79 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
Molarity Calculator
Reconstitution Calculator
Dilution Calculator
Product Datasheets
References
References are publications that support the products' biological activity.
Cosenza et al (2000) Locomotor activity and occupancy of brain cannabinoid CB1 receptors by the antagonist/inverse agonist AM281. Synapse 38 477 PMID: 11044895
Gifford et al (1997) Effect of the cannabinoid receptor SPECT agent, AM 281, on hippocampal acetylcholine release from rat brain slices. Neurosci.Lett. 238 84 PMID: 9464661
Gatley et al (1998) Imaging the brain marijuana receptor: development of a radioligand that binds to cannabinoid CB1 receptors in vivo. J.Neurochem. 70 417 PMID: 9422389
Lan et al (1999) Design and synthesis of the CB1 selective cannabinoid antagonist AM281: a potential human SPECT ligand. AAPS Pharmsci. 1 E4 PMID: 11741201
Keywords: AM 281, supplier, Potent, selective, CB1, antagonists, inverse, agonists, Cannabinoids, Receptors, AM281, cb1r, CB1, Receptors, CB1, Receptors, Tocris Bioscience
