Pravadoline (WIN 48098) is an antiinflammatory and analgesic compound with an IC50 of 4.9 uM for inhibition of the synthesis of prostaglandins (PGs) in mouse brain. Pravadoline (WIN 48098) is related in structure to non-steroidal antinflammtory agents such as indometacin. Pravadoline (WIN 48098) was developed in the 1980s as a new antiinflammatory and prostaglandin synthesis inhibitor, acting through inhibition of the enzyme cyclooxygenase (COX).
|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.
|Source||Org Lett (2016). Scheme 1. WIN 48098 (Abmole Bioscience Inc.)|
|Results||This new synthetic method provides a short synthesis of pravadoline 7a (WIN 48098) that acts as a potent antiinflammatory and analgesic drug (IC50 4.9 μM, Ki 2511 nM at CB1).|
Org Lett 2016 Feb 5;412-5.
[3 + 2]-Annulations of N-Hydroxy Allenylamines with Nitrosoarenes: One-Pot Synthesis of Substituted Indole Products.
Pravadoline purchased from AbMole
|Related COX Products|
Vitamin E is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.
Tenoxicam is a good HO. radicals scavenger with an IC50 of 56.7 μM.
Suprofen is a dual COX-1/COX-2 inhibitor, used as a non-steroidal anti-inflammatory analgesic and antipyretic.
Salicylic acid is a beta hydroxy acid that occurs as a natural compound in plants which is an inhibitor of ethylene biosynthesis and cyclooxygenase activity.
Propyphenazone is a pyrazolone derivative with anti-inflammatory, analgesic and antipyretic activity, Propyphenazone-based analogues as prodrugs and selective cyclooxygenase-2 inhibitors.
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