Acetaminophen is a highly selective inhibitor of COX-2 and 6-keto-PGF1 alpha with IC50 of 302.3 mg/kg and 10 uM, respectively. Administration of high-dose AAP [302.3 mg/kg (IC50 for COX-2)] or PHE [179.2 mg/kg (IC50 for COX-2)] and of non-specific (indomethacin: 20 mg/kg) or specific COX-2 (NS-398: 10 mg/kg) inhibitor impaired the performance in hidden platform (HP) not visible platform (VP) tasks, whereas low-dose (15.1 mg/kg) AAP facilitated performance in HP and VP tasks. Nanomolar concentrations of peroxynitrite increased the activity of isolated PGHS and prostacyclin formation by aortic endothelial cells. This elevated activity was efficiently inhibited by pharmacologically relevant concentrations of acetaminophen (IC50 approximately 10 uM for 6-keto-PGF1alpha) and other free radical scavengers.
*The compound is unstable in solutions, freshly prepared is recommended
Molecular Weight | 151.16 |
Formula | C8H9NO2 |
CAS Number | 103-90-2 |
Solubility (25°C) | DMSO 20 mg/mL Water 8 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.
[1] Clyde J Wright. Acetaminophen and the Developing Lung: Could There Be Lifelong Consequences?
[3] Anita Aminoshariae, et al. Acetaminophen: old drug, new issues
[4] K Brune, et al. Acetaminophen/paracetamol: A history of errors, failures and false decisions
[5] Marta Jźwiak-Bebenista, et al. Paracetamol: mechanism of action, applications and safety concern
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