Mayumi Yamamura

TL;DR: The rapid disappearance of the (S)-enantiomer from the plasma was thought to be due to the rapid metabolism of the (+/-)-4-cyanoanilino)-5,6-dihydro-7-hydroxy-7H-cyclopenta[d]pyrimidine by different drug-metabolizing enzymes, depending on species.

TL;DR: In vitro results were in good accordance with previously reported in vivo excretion data of the 2‐keto metabolite and the non‐detectable plasma concentrations of the (S)‐enantiomer in monkeys and humans after administration of racemic RS‐8359.

TL;DR: No small discrepancy existed in the almost negligible catalytic activity and the fairly high expression levels of protein and mRNA in the F344/DuCrj and Slc:Wistar strain rats, but some genetic factors might possibly be one of reasons for the discrepancy.

TL;DR: Plasma concentrations of the [R] and [S]-enantiomers of RS-8359 were determined by chiral column HPLC after oral administration of each enantiomer to rats, mice, dogs, and monkeys, and it was found that plasma concentrations were markedly lower than those of the (R) to [S] chiral inversion.

TL;DR: A method for the quantitative determination of the eight diol stereoisomers excreted in urine after administration of CS-670(I) is reported, which suggested the chiral inversion from cis-OH to trans-OH was suggested to occur through the saturated ketone intermediate.