Electric Literature of 102089-74-7, As a society publisher, everything we do is to support the scientific community – so you can trust us to always act in your best interests, and get your work the international recognition that it deserves. 102089-74-7, Name is Boc-D-Phenylglycinol, SMILES is [C@@H](NC(OC(C)(C)C)=O)(C1=CC=CC=C1)CO, belongs to phthalazine compound. In a article, author is Akabane, Takafumi, introduce new discover of the category.
Human hepatocytes are a physiologically relevant tool useful in evaluating liver-related pharmacokinetics, including non-cytochrome P-450 (CYP) metabolism, due to their broad spectrum of metabolic enzyme activity. To verify the usefulness of human hepatocytes in evaluating non-CYP metabolism for drug discovery, we compared intrinsic clearance values (CLint) in freshly isolated and cryopreserved hepatocytes using 14 compounds primarily metabolized by non-CYP enzymes, including UDP-glucuronosyltransferase, carbonyl/aldo-keto reductase, aldehyde oxidase, flavin-containing monooxygenase, and monoamineoxidase. Cryopreservation resulted in a > 20% reduction (maximum: 50%) in CLint in 7/14 compounds (statistically significant for 5 compounds) on comparing CLint values in freshly isolated and cryopreserved hepatocytes from the same donors (n = 4). However, the number of compounds with > 20% CLint reduction decreased to 3 on comparing average of CLint values including un-matched donors (dolasetron: -27%, naltorexone: -32%, and phthalazine: -48%; statistically significant for phthalazine, n = 6-11). These findings suggest that fresh hepatocytes are useful in evaluating intact non-CYP enzyme activities. However, we must note that the reduction in CLint by cryopreservation could be rendered negligible if high-activity lots are selected for assay. We therefore recommend using cryopreserved hepatocytes for large-scale screening for non-CYP metabolism in drug discovery research considering the advantages in usability with cryopreserved hepatocytes.
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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem