CYP3A4 can N-demethylate loperamide

Stable Identifier
R-HSA-211948
Type
Reaction [transition]
Species
Homo sapiens
Compartment
endoplasmic reticulum membrane, endoplasmic reticulum lumen
ReviewStatus
5/5
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CYP3A4 can N-demethylate loperamide
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The CYP3A family are the most abundantly expressed P450s in human liver, accounting for around 50% of xenobiotic drug metabolism. CYP3A4 is the most abundant member of the family and possesses broad specificity to a range of xenobiotics. Loperamide (LOP), an antidiarrheal, is mainly metabolized to desmethylloperamide (DLOP) through the N-demethylation pathway. This initial N-demethylation is carried out by CYP3A4.
Literature References
PubMed ID Title Journal Year
15365656 Identification of cytochrome P450 isoforms involved in the metabolism of loperamide in human liver microsomes

Kim, KA, Chung, J, Jung, DH, Park, JY

Eur J Clin Pharmacol 2004
Participants
Input
Output
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as an event of
Catalyst Activity

monooxygenase activity of Cytochrome P450 (CYPIIIA4 based) [endoplasmic reticulum membrane]

Physical Entity
Cytochrome P450 (CYPIIIA4 based) [endoplasmic reticulum membrane] (Homo sapiens)
Activity
monooxygenase activity (GO:0004497)
Orthologous Events
CYP3A4 can N-demethylate loperamide (Bos taurus)
CYP3A4 can N-demethylate loperamide (Canis familiaris)
CYP3A4 can N-demethylate loperamide (Danio rerio)
CYP3A4 can N-demethylate loperamide (Gallus gallus)
CYP3A4 can N-demethylate loperamide (Mus musculus)
CYP3A4 can N-demethylate loperamide (Rattus norvegicus)
CYP3A4 can N-demethylate loperamide (Sus scrofa)
CYP3A4 can N-demethylate loperamide (Xenopus tropicalis)
Authored
Jassal, B  (2008-05-19)
Reviewed
D'Eustachio, P  (2008-05-28)
Created
Jassal, B  (2008-02-08)
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