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Oxethazaine

Cat. No. M2906
Oxethazaine Structure
Synonym:

Oxethacaine

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Biological Activity

Oxethazaine is a strong local anaesthetic, which acts in a number of ways to numb the walls of the stomach and relieve the pain associated with hyperacidic conditions. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis.

Chemical Information
Molecular Weight 467.64
Formula C28H41N3O3
CAS Number 126-27-2
Solubility (25°C) DMSO 50 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Hokuto Namba, et al. Inhibitory Effect of Oxethazaine on Midazolam Metabolism in Rats

[2] Andressa R Prado, et al. Complexation of oxethazaine with 2-hydroxypropyl-β-cyclodextrin: increased drug solubility, decreased cytotoxicity and analgesia at inflamed tissues

[3] Lin Zhang, et al. Oxethazaine inhibits hepatitis B virus capsid assembly by blocking the cytosolic calcium-signalling pathway

[4] Soo-Yeun Lee, et al. The abuse potential of oxethazaine: effects of oxethazaine on drug-seeking behavior and analysis of its metabolites in plasma and hair in animal models

[5] Mei-Chich Hsu, et al. Oxethazaine as the source of mephentermine and phentermine in athlete's urine

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