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Chemical Compound Review:

AG-J-29922 1-butyl-3-[4-(hydroxymethyl) phenyl]sulfony...

Synonyms: CHEBI:63799, UC160_SIGMA, HMDB06408, SureCN14067598, CTK8G0233, ...

Miners, J.O. et al., Veronese, M.E. et al., Braselton, W.E. et al., Wang, J.S. et al., Zhu-Ge, J. et al.

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High impact information on Hydroxytolbutamide

It consists of formation of the thermally stable methyl-trifluoroacetyl derivatives of chlorpropamide and tolbutamide, and the methyl-heptafluorobutyryl derivatives of hydroxymethyltolbutamide and carboxytolbutamide, which are then analyzed by electron-capture gas chromatography [1].
Plasma tolbutamide clearance and half-life were measured, as were the metabolic ratio (hydroxytolbutamide + carboxytolbutamide/tolbutamide) in successive 6-hour urine collections [2].
The effect of human serum albumin (Hsa) and human liver cytosol (Hlc) on the in vitro enzyme kinetics of the formation of hydroxytolbutamide (CYP2C9 marker reaction) and the inhibitory effect of gemfibrozil on tolbutamide hydroxylation were examined using human liver microsomes [3].
Anti-human liver NADPH-cytochrome P-450 reductase IgG inhibited hydroxytolbutamide formation and this metabolite was not formed when NADPH-generating system was omitted from microsomal incubations [4].
A range of clinically used drugs and xenobiotics used as probes for cytochrome P-450 activity in laboratory animals was screened for inhibitory effects on hydroxytolbutamide formation [4].

Anatomical context of Hydroxytolbutamide

The S9 fraction of the established cell line metabolizes tolbutamide to hydroxytolbutamide [5].

Analytical, diagnostic and therapeutic context of Hydroxytolbutamide

Tolbutamide, hydroxytolbutamide, and carboxytolbutamide in urine were determined by newly developed HPLC procedures [2].

References

Measurement of antidiabetic sulfonylureas in serum by gas chromatography with electron-capture detection. Braselton, W.E., Bransome, E.D., Huff, T.A. Diabetes (1977) [Pubmed]
Validation of the tolbutamide metabolic ratio for population screening with use of sulfaphenazole to produce model phenotypic poor metabolizers. Veronese, M.E., Miners, J.O., Randles, D., Gregov, D., Birkett, D.J. Clin. Pharmacol. Ther. (1990) [Pubmed]
Effect of albumin and cytosol on enzyme kinetics of tolbutamide hydroxylation and on inhibition of CYP2C9 by gemfibrozil in human liver microsomes. Wang, J.S., Wen, X., Backman, J.T., Neuvonen, P.J. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
Tolbutamide hydroxylation by human liver microsomes. Kinetic characterisation and relationship to other cytochrome P-450 dependent xenobiotic oxidations. Miners, J.O., Smith, K.J., Robson, R.A., McManus, M.E., Veronese, M.E., Birkett, D.J. Biochem. Pharmacol. (1988) [Pubmed]
Establishment of a transgenic cell line stably expressing human cytochrome P450 2C18 and identification of a CYP2C18 clone with exon 5 missing. Zhu-Ge, J., Yu, Y.N., Qian, Y.L., Li, X. World J. Gastroenterol. (2002) [Pubmed]

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