PMID-sentid Pub_year Sent_text comp_official_name comp_offsetprotein_name organism prot_offset 10570018-0 1999 Azelastine N-demethylation by cytochrome P-450 (CYP)3A4, CYP2D6, and CYP1A2 in human liver microsomes: evaluation of approach to predict the contribution of multiple CYPs. azelastine 0-10 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 57-63 11948533-3 2002 Because we previously clarified that azelastine, an antiallergy and antiasthmatic drug, is N-demethylated by CYP1A2, CYP2D6, and CYP3A4 in humans, the reaction was used as a model. azelastine 37-47 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 117-123 10570018-3 1999 In microsomes from human B-lymphoblast cells, recombinant cytochrome P-450 (CYP)2D6 and CYP1A1 exhibited higher azelastine N-demethylase activity than did other CYP enzymes. azelastine 112-122 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 58-83 10570018-4 1999 On the other hand, recombinant CYP3A4 and CYP1A2 as well as CYP1A1 and CYP2D6 in microsomes from baculovirus-infected insect cells were active in azelastine N-demethylation. azelastine 146-156 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 71-77 10570018-12 1999 Summarizing the results, azelastine N-demethylation in humans liver microsomes is catalyzed mainly by CYP3A4 and CYP2D6, and CYP1A2 to a small extent (in average, 76.6, 21.8, and 3.9%, respectively), although the percent contribution of each isoform varied among individuals. azelastine 25-35 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 113-119 10383922-12 1999 Among the human CYPs tested, the inhibitory effects of azelastine and its two metabolites were the most potent on human CYP2D6. azelastine 55-65 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 120-126 9506001-7 1997 Azelastine did not inhibit CYP3A4 activity but it did inhibit CYP2D6 and CYP2C19 activity with Ki values exceeding maximum plasma concentration by 120 to 800-fold. azelastine 0-10 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 62-68 10421623-8 1999 These observations suggested that the N-demethylation of azelastine is most extensively catalyzed by the CYP2D6 and 3A4 isoforms in humans. azelastine 57-67 cytochrome P450 family 2 subfamily D member 6 Homo sapiens 105-111