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
|Source||Neuron (2020 Feb). Figure 3. SR 141716A (Abmole Bioscience)|
|Results||Inhibiting CB1R with SR at ZT0 increased inhibitory transmission to ZT12 levels, while SR had no effect at ZT12.|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 25 mg/mL|
Selective antagonism of the anticonvulsant effects of felbamate by glycine.
Coffin, et al. Eur J Pharmacol. 1994;256: R9. PMID: 8050461.
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