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Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24). Org 27569 inhibits CB1 receptor antagonist efficacy in vitro (pKb = 7.57). Org 27569 binds to a regulatory site on the CB1 receptor target, causing a conformational change that increases the binding affinity of CB1 agonists such as CP 55,940, while decreasing the binding affinity of CB1 antagonists or inverse agonists such as rimonabant. Org 27569 significantly increases binding of the CB1 agonist [3H]CP 55.940 (pKb = 5.67) and decreases binding of the CB1 inverse agonist [3H]SR 141716A (pKb = 5.95), and so in practice behaves as an insurmountable antagonist of CB1 receptor function.
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells expressing the wild-type (●), T210I (△), and T210A (■) receptors |
| Preparation method | GTPγS Binding Assay 15 μg of membranes were incubated for 60 min at 30 °C in a total volume of 500 μM GTPγS binding assay buffer (50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, and 100 mM NaCl) with unlabeled ligand (at least nine different concentrations were used ranging between 100 pM and 100 μM), 0.1 nM [35S]GTPγS (1250 Ci/mmol), 10 μM GDP, and 0.1% (w/v) BSA. The basal GTPγS binding was measured in the absence of ligand. Nonspecific binding was determined with 10 μM unlabeled GTPγS. The reaction was terminated by rapid filtration through Whatman GF/C filters. The radioactivity trapped in the filters was determined by liquid scintillation counting. |
| Concentrations | 0~10 μ M |
| Incubation time | 5~15 min |
| Animal Experiment | |
|---|---|
| Animal models | Adult male Sprague–Dawley rats |
| Formulation | a mixture of 1 part absolute ethanol, 1 part Emulphor-620, and 18 parts physiological saline |
| Dosages | 8 days of daily 5.6 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 409.95 |
| Formula | C24H28ClNO3 |
| CAS Number | 868273-06-7 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Cannabinoid Products |
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| AM-2201
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| AM251
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| BML-190
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