BAY-59-3074 is a novel cannabinoid CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors, respectively. BAY 59-3074 (0.3-3 mg/kg, p.o.) induce antihyperalgesic and antiallodynic effects against thermal or mechanical stimuli in rat models of chronic neuropathic. Antiallodynic efficacy of BAY 59-3074 (1 mg/kg, p.o.) in the spared nerve injury model was maintained after 2 weeks of daily administration. However, tolerance developed rapidly (within 5 days) for cannabinoid-related side effect. BAY 59-3074 have analgesic, antihyperalgesic, and antiallodynic properties in rat models of acute and chronic pain.
|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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO: 30 mg/mL|
Conformationally constrained analogs of BAY 59-3074 as novel cannabinoid receptor ligands.
Teng H, et al. Bioorg Med Chem Lett. 2011 Oct 1;21(19):5999-6002. PMID: 21880487.
3-[2-cyano-3-(trifluoromethyl)phenoxy]phenyl-4,4,4-trifluoro-1-butanesulfonate (BAY 59-3074): a novel cannabinoid Cb1/Cb2 receptor partial agonist with antihyperalgesic and antiallodynic effects.
De Vry J, et al. J Pharmacol Exp Ther. 2004 Aug;310(2):620-32. PMID: 15140913.
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