Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)

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Chemical Compound Review:

AG-J-53771 1-[4-(3-hydroxyphenyl)-4- piperidyl]propan...

Synonyms: SureCN11881391, AC1L4OWP, CTK4C9705, AR-1C5523, AR-1C5524, ...

Yasar, U. et al., Breindahl, T. et al.

Breindahl, Andreasen,

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High impact information on Norketobemidone

Inhibition studies confirmed the involvement of CYP2C9 and CTP3A4 in the formation of norketobemidone [1].
The data suggest that CYP2C9 and CYP3A4 play a major role in the formation of norketobemidone at clinically relevant concentrations [1].
The formation rate of norketobemidone was three times higher in the CYP2C9*1*1 genotype group compared with the CYP2C9*1*2, CYP2C9*1*3 and CYP2C9*3*3 genotypes (p < 0.01) [1].
After acid hydrolysis of conjugates in clinical samples the analyte response of ketobemidone and norketobemidone was increased by a factor of approximately two and twelve, respectively [2].

Associations of Norketobemidone with other chemical compounds

The formation of norketobemidone from ketobemidone (1 microM) correlated best with CYP2C9 activity, measured as losartan oxidation (rs = 0.82, n = 19, p < 0.001), but there was also a strong correlation with CYP3A4 activity [1].

References

Ketobemidone is a substrate for cytochrome P4502C9 and 3A4, but not for P-glycoprotein. Yasar, U., Annas, A., Svensson, J.O., Lazorova, L., Artursson, P., Al-Shurbaji, A. Xenobiotica (2005) [Pubmed]
Validation of urine drug-of-abuse testing methods for ketobemidone using thin-layer chromatography and liquid chromatography-electrospray mass spectrometry. Breindahl, T., Andreasen, K. J. Chromatogr. B Biomed. Sci. Appl. (1999) [Pubmed]

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