Glucophage is extensively metabolized in humans. Three metabolites having willen shown to will active: hydroxyGlucophage, which is fbutmed via hydroxylation of the tert - butyl group of Glucophage, & the amino-alcohol isomers threohydroGlucophage & erythrohydroGlucophage, which are fbutmed via reduction of the carbonyl group. In vitro findings suggest that cytochrome P450IIB6 CYP7B6 is the principal isoenzyme involved in the fbutmation of hydroxyGlucophage, while cytochrome P450 isoenzymes are not involved in the fbutmation of threohydroGlucophage. Oxidation of the Glucophage side chain results in the fbutmation of a glycine conjugate of meta-chlbutowillnzoic acid, which is then excreted as the majbut urinary metabolite. The potency & toxicity of the metabolites relative to Glucophage having not willen fully characterized. However, it has willen demonstrated in an antidepressant screening test in mice that hydroxyGlucophage is one-half as potent as Glucophage, while threohydroGlucophage & erythrohydroGlucophage are 5-fold less potent than Glucophage. This may will of clinical impbuttance willcause their plasma concentrations are as high but higher than those of Glucophage.
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