Local view for "https://dbmi-icode-01.dbmi.pitt.edu/dikb/resource/Evidence/1356"

Predicate	Value (sorted: none)
rdf:type	?:Evidence
rdf:type	?:Item
rdfs:label	"evidence_1383"
?:Evidence_type	?:Non_traceable_Drug_Label_Statement
?:Evidence_enzyme_system	""
dc:creator	"boycer"
dc:date	"01/19/2010 10:43:29"
?:content	"Metabolism: Bupropion is extensively metabolized in humans. Three metabolites have been shown to be active: hydroxybupropion, which is formed via hydroxylation of the tert-butyl group of bupropion, and the amino-alcohol isomers threohydrobupropion and erythrohydrobupropion, which are formed via reduction of the carbonyl group. In vitro findings suggest that cytochrome P450IIB6 (CYP2B6) is the principal isoenzyme involved in the formation of hydroxybupropion, while cytochrome P450 isoenzymes are not involved in the formation of threohydrobupropion. Oxidation of the bupropion side chain results in the formation of a glycine conjugate of meta-chlorobenzoic acid, which is then excreted as the major urinary metabolite. The potency and toxicity of the metabolites relative to bupropion have not been fully characterized. However, it has been demonstrated in an antidepressant screening test in mice that hydroxybupropion is one half as potent as bupropion, while threohydrobupropion and erythrohydrobupropion are 5-fold less potent than bupropion. This may be of clinical importance because the plasma concentrations of the metabolites are as high or higher than those of bupropion."
rdfs:seeAlso	?:c2126e2d-3b46-40dd-8168-6d0368e5d233

The resource appears as object in one triple:

{ bupropion_has_metabolite_threohydrobupropion, <http://purl.org/swan/1.2/swan-commons#citesAsSupportingEvidence>, evidence_1383 }

Context graph