| Name | CB1 antagonist 4 |
| Description | CB1 antagonist 4 is an antagonist of cannabinoid receptor type 1 (CB1), with potential for the treatment of obesity and type 2 diabetes. |
| In vivo | CB1 antagonist 4, a novel, largely peripherally restricted CB1 antagonist, in terms of fear-promoting consequences of systemic vs. intracerebral injections.Different groups of male C57BL/6 N mice underwent auditory fear conditioning, followed by re-exposure to the tone.Mice were treated per os (p.o.) with CB1 antagonist 4 (10, 30, or 100 mg/kg), rimonabant (10 mg/kg;a brain penetrating CB1 antagonist/inverse agonist which served as a positive control), or vehicle, 2 h prior the tone presentation.Only the high dose of CB1 antagonist 4 (100 mg/kg) induced a significant increase in freezing behavior, similar to that induced by rimonabant (10 mg/kg) (p <0.001).?If injected into the brain both CB1 antagonist 4 (10 or 30 μg/mouse) and rimonabant (1 or 10 μg/mouse) caused a sustained fear response to the tone, which was more pronounced after rimonabant treatment.Taken together, CB1 antagonist 4 was at least one order of magnitude less effective in promoting fear responses than rimonabant.Given the equipotency of the two CB1 antagonists with regard to weight loss and metabolic syndrome-like symptoms in rodent obesity models, our results point to a critical dose range in which CB1 antagonist 4 might be beneficial for indications such as obesity and metabolic disorders with limited risk of fear-promoting effects[1]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 40 mg/mL (64.77 mM), Sonication is recommended.
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| Keywords | peripheral | Cannabinoid Receptor | CB1 | TM-38837 | antiobesity | TM 38837 | TM38837 | inhibit | fat | Inhibitor | metabolic | fear |
| Inhibitors Related | β-Caryophyllene | CB2 modulator 1 | Pregnenolone | Pregnenolone acetate | CB1 antagonist 2 | OMDM-5 | CB2 receptor agonist 2 | 2,3-Butanediol | Drinabant | AM281 |
| Related Compound Libraries | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | Anti-Diabetic Compound Library | Anti-Obesity Compound Library | Inhibitor Library | NO PAINS Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | GPCR Compound Library |
United States
