Title : Stereoselective Bupropion Hydroxylation by Cytochrome P450 CYP2B6 and Cytochrome P450 Oxidoreductase Genetic Variants.

Pub. Date : 2020 Jun

PMID : 32238417






12 Functional Relationships(s)
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1 Stereoselective bupropion hydroxylation by cytochrome P450 CYP2B6 and cytochrome P450 oxidoreductase genetic variants. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
2 Bioactivation of the antidepressant and smoking cessation drug bupropion is catalyzed predominantly by cytochrome P4502B6 (CYP2B6). Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
3 Bioactivation of the antidepressant and smoking cessation drug bupropion is catalyzed predominantly by cytochrome P4502B6 (CYP2B6). Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
4 Bupropion hydroxylation is the canonical in vitro and in vivo probe for CYP2B6 activity. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
5 Some CYP2B6 variants affect bupropion disposition. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
6 This investigation evaluated the influence of several human CYP2B6 and POR genetic variants on stereoselective bupropion metabolism, using an insect cell coexpression system containing CYP2B6, POR and cytochrome b5. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
7 CYP2B6-catalyzed bupropion hydroxylation is stereoselective. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
8 Established concordance between human bupropion hydroxylation in vitro and in vivo, together with these new results, suggests additional CYP2B6 variants may influence human bupropion disposition. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
9 Established concordance between human bupropion hydroxylation in vitro and in vivo, together with these new results, suggests additional CYP2B6 variants may influence human bupropion disposition. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
10 SIGNIFICANCE STATEMENT: Bupropion pharmacokinetics, metabolism and clinical effects are affected by the CYP2B6*6 polymorphism. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
11 Other expressed CYP2B6 polymorphisms had diminished (*5, *6, *7, *9, *19, *26) or defective (*16, *18) in vitro bupropion hydroxylation. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens
12 These CYP2B6 polymorphisms may portend diminished in vivo bupropion hydroxylation and predict additional clinically important variant alleles. Bupropion cytochrome P450 family 2 subfamily B member 6 Homo sapiens