Characterization of plasma protein binding in two mouse models of humanized liver, PXB mouse and humanized TK-NOG mouse.

The unbound fractions in plasma ( ) in two mouse models of humanized liver mice, PXB and humanized TK-NOG mice, were compared with human values using equilibrium dialysis method. A good relationship between values obtained from PXB mice and humans was observed; the of 34/39 compounds (87.2%) in PXB mice were within 3-fold of human .

Prediction of human pharmacokinetics of long half-life compounds using chimeric mice with humanised liver.

1. The prediction of human pharmacokinetic (PK) parameters is an important theme to select drug candidates from preclinical studies. It is essential to improve the prediction accuracy of compound half-life () in humans.

Application of unbound liver-to-plasma concentration ratio to quantitative projection of cytochrome P450-mediated drug-drug interactions using physiologically based pharmacokinetic modelling approach.

1. This study evaluated the prediction accuracy of cytochrome P450 (CYP)-mediated drug-drug interaction (DDI) using minimal physiologically-based pharmacokinetic (PBPK) modelling incorporating the hepatic accumulation factor of an inhibitor (i.e.

EEG Correlates of the Flow State: A Combination of Increased Frontal Theta and Moderate Frontocentral Alpha Rhythm in the Mental Arithmetic Task.

Flow experience is a subjective state experienced during holistic involvement in a certain activity, which has been reported to function as a factor promoting motivation, skill development, and better performance in the activity. To verify the positive effects of flow and develop a method to utilize it, the establishment of a reliable measurement of the flow state is essential. The present study utilized an electroencephalogram (EEG) during an experimentally evoked flow state and examined the possibility of objective measurement of immediate flow.

Comparison of predictability for human pharmacokinetics parameters among monkeys, rats, and chimeric mice with humanised liver.

1. The aim of the present study was to evaluate the usefulness of chimeric mice with humanised liver (PXB mice) for the prediction of clearance (CL) and volume of distribution at steady state (Vd), in comparison with monkeys, which have been reported as a reliable model for human pharmacokinetics (PK) prediction, and with rats, as a conventional PK model. 2.

Development and characterization of microsatellite loci in Ixeridium dentatum (Asteraceae, Lactuceae).

We isolated and characterized seven microsatellite loci for the perennial herb Ixeridium dentatum ssp. dentatum, an apomictic triploid distributed throughout the lowland areas of East Asia. The number of alleles ranged from two to seven in 32 screened individuals of I.

Dissociation of DNA from histone by reaction of anti-cancer drug cis-diamminedichloroplatinum(II) with DNA-histone complexes used as cellular model.

Although both cis-diamminedichloroplatinum(II) (cisplatin or cis-DDP) and trans-diamminedichloroplatinum(II) bind to DNA, only cis-DDP is widely used as a chemotherapeutic agent; the stereoisomer trans-DDP is inactive. DNA, generally, is wound around the histone core in the nucleus of living cells and forms the nucleosome structure. To understand the essentially different anticancer activities of cis-DDP and trans-DDP, it is necessary to investigate the interaction of cis-DDP (or trans-DDP) with DNA around the histone in the nucleosome.

DNA topology: topological transformation of DNA by reaction of cisplatin-DNA-core histone complexes with human DNA topoisomerase.

Cis-diamminedichloroplatinium(II), an active antitumor agent binds to core-histone -SV40 DNA complexes prepared by reaction of DNA with core-histone, and alters the fiber-like structure into the loosened structure. In order to model the cisplatin-modified chromatin complexes in cell, the complexes were reacted with human DNA topo II. We found the generations of unique topologically isomers such as trefoil knot (and catenane) and pseudo catenane (and pseudo knot) by reaction of cis-DDP--linearDNA--core-histone complexes with DNA topo I.