Pub. Date : 1998 May
PMID : 9580580
5 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
| 1 | The formation rate of DHPBI from 25 microM pimozide in nine human livers correlated significantly with the catalytic activity of CYP3A (Spearman r = 0.79, P = .028), but not with other isoforms. | Pimozide | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 2 | Recombinant human CYP3A4 catalyzed DHPBI formation from 10 microM pimozide at the highest rate (V = 2.2 +/- 0.89 pmol/min/pmol P450) followed by CYP1A2 (V = 0.23 +/- 0.08 pmol/min/pmol P450), but other isoforms tested did not. | Pimozide | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 3 | Pimozide itself was a potent inhibitor of CYP2D6 in HLMs when preincubated for 15 min (Ki = 0.75 +/- 0.98 microM) and a moderate inhibitor of CYP3A (Ki = 76.7 +/- 34.5 microM), with no significant effect on other isoforms tested. | Pimozide | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 4 | Our results suggest that pimozide metabolism is catalyzed mainly by CYP3A, but CYP1A2 also contributes. | Pimozide | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |
| 5 | Pimozide metabolism is likely to be subject to interindividual variability in CYP3A and CYP1A2 expression and to drug interactions involving these isoforms. | Pimozide | cytochrome P450 family 3 subfamily A member 4 | Homo sapiens |