Chemical research careers are more diverse than they might first appear, as there are many different reasons to conduct research and many possible environments. , Synthetic Route of 1439-36-7, and the best way to enjoy it and learn about it is performing experiments.Introducing a new discovery about 1439-36-7, Name is 1-(Triphenylphosphoranylidene)propan-2-one, molecular formula is C21H19OP, belongs to phthalazine compound. In a document, author is Akabane, Takafumi.
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