in vivo: Given at equianalgesic doses, morphine (3.5 mg/kg i.v.) significantly lowers the pO2 over 20 mm Hg and raises the pCO2 over 10 mm Hg as measured in arterial blood samples, whereas meptazinol (10 mg/kg i.v.) has no significant effects on either. The group receiving meptazinol demonstrated no cardiovascular changes although bispectral index dropped by an additional 19% when compared to 1 min after barbiturate injection . Rapid and significant levels of MEP in plasma and CSF can be achieved after nasal administration whereas the oral administration resulted in considerably lower drug concentrations.
In Vitro
in vitro: Meptazinol inhibits a portion of 3H-labeled opiate and opioid peptide binding quite potently, with IC50 value under 1 nM.
Kinase Assay
Cell Assay
Animal Administration
References
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