Rimonabant Hydrochloride (SR 141716A) is a potent and selective cannabinoid CB1 receptor antagonist (Ki = 1.98 nM). Rimonabant Hydrochloride also acts as an inverse agonist reversing adenylyl cyclase inhibition by WIN 55,212-2 (IC50 = 48 nM). Rimonabant Hydrochloride displays no activity at CB2 receptors. Rimonabant Hydrochloride (SR 141716A) reduces food intake and body weight in orally dosed non-obese Wistar rats.
Neuron. 2020 Feb 19;105(4):621-629.e4.
Daily Oscillation of the Excitation-Inhibition Balance in Visual Cortical Circuits.
Rimonabant Hydrochloride purchased from AbMole
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Source | Neuron (2020 Feb). Figure 3. SR 141716A (Abmole Bioscience) |
| Method | sIPSC assay | |
| Cell Lines | mice | |
| Concentrations | 10 μM | |
| Incubation Time | 1h | |
| Results | Inhibiting CB1R with SR at ZT0 increased inhibitory transmission to ZT12 levels, while SR had no effect at ZT12. |
| Molecular Weight | 500.25 |
| Formula | C22H21Cl3N4O.HCl |
| CAS Number | 158681-13-1 |
| Solubility (25°C) | DMSO 25 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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