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URB597 is a relatively selective fatty acid amide hydrolase (FAAH) inhibitor with IC50 of 4.6 and 0.5 nM in brain membranes and intact neurons, respectively. FAAH is the primary degradatory enzyme for the endocannabinoid anandamide and, as such, inhibition of FAAH leads to an accumulation of anandamide in the CNS and periphery where it activates cannabinoid receptors. URB597 ?produced measurable antidepressant and analgesic effects by increasing endocannabinoids. URB597 ?shows both anti-nociceptive and anxiolytic effects in vivo but not evokes other symptoms associated with cannabinoid-like compounds. Hence, URB597 may provide a new strategy for the treatment of pain and anxiety.
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Source | Cell Physiol Biochem (2018). Figure 1. URB597 |
| Method | injections | |
| Cell Lines | WKY rats | |
| Concentrations | 1mg/kg | |
| Incubation Time | two weeks | |
| Results | Interestingly, chronic URB597 administration significantly increased intramyocardial glycogen level in the DOCA-salt rats compared to the hypertensive group alone |
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Adult male Wistar rats (250–300 g) and C57/BL6 or FAAH-/- mice |
| Formulation | sterile 0.9% sodium chloride solution |
| Dosages | 0.3 mg/kg |
| Administration | Inject subcutaneously in a single dose 2 hours or 16 hours before killing |
| Molecular Weight | 338.4 |
| Formula | C20H22N2O3 |
| CAS Number | 546141-08-6 |
| Solubility (25°C) | DMSO 58 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[5] Stephen G Woodhams, et al. The cannabinoid system and pain
| Related FAAH Products |
|---|
| JP104
JP104, a aryl carbamate, is an irreversible FAAH inhibitor with a pIC50 of ~8. |
| AM1172
AM1172 is metabolically stable anandamide uptake inhibitor and FAAH inhibitor. |
| URB937
URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. |
| JNJ-40355003
JNJ-40355003 is a potent and selective atty acid amide hydrolase (FAAH) inhibitor. |
| N-Benzyllinolenamide
N-Benzyllinolenamide is a natural macamide isolated from Lepidium meyenii, acts as an inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 of 41.8 μM. |
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