Pharmacokinetics and disposition of dalcetrapib in rats and monkeys.

1. The pharmacokinetics and metabolism of dalcetrapib (JTT-705/RO4607381), a novel cholesteryl ester transfer protein inhibitor, were investigated in rats and monkeys. 2.

In vitro experimental system for evaluating inhibitory effect of investigational drugs on P-glycoprotein-mediated transcellular transport of tacrolimus (FK506).

In this study, an in vitro experimental system for evaluating the inhibitory effect of investigational drugs on the P-glycoprotein (P-gp, MDR1)-mediated transport of tacrolimus (FK506) was developed using LLC-PK1-MDR1 and LLC-PK1 wild-type (control) cells. The amount of tacrolimus (concentrations: 1 and 5 μm) transported into P-gp-expressing and control cells increased with time in both the apical-to-basal and basal-to-apical directions at incubation times ranging from 40 min to 2 h. The corrected apparent permeability (Papp) ratio, obtained by dividing the Papp ratio in P-gp-expressing cells by that in the control cells, ranged from 2.

Intestinal absorption mechanism of mirabegron, a potent and selective β₃-adrenoceptor agonist: involvement of human efflux and/or influx transport systems.

Mirabegron, a weak-basic compound, is a potent and selective β3-adrenoceptor agonist for the treatment of overactive bladder. Mirabegron extended release formulation shows dose-dependent oral bioavailability in humans, which is likely attributable to saturation of intestinal efflux abilities leading to higher absorption with higher doses. This study evaluated the membrane permeability of mirabegron and investigated the involvement of human intestinal transport proteins in the membrane permeation of mirabegron.

Intracavity second-harmonic generation at 320 nm of an actively Q-switched Pr:LiYF4 laser.

We demonstrate pulse laser operation of a Pr:LiYF(4) laser pumped by InGaN laser diodes (444 nm) using an acousto-optic modulator. We obtained a maximum laser peak power of 167 W (4 μJ/pulse) with a pulse width of 24 ns at an 11 kHz repetition rate for a 63 nm wavelength. Employing an 8 mm long lithium triborate nonlinear crystal in the laser cavity, we obtained a maximum peak power of 55 W (2.

Nucleophilic deoxyfluorination of catechols.

Nucleophilic deoxyfluorinaiton of one of the two hydroxyl groups of catechols has been developed via the Umpolung concept. This method was successively applied to naturally occurring catechols, such as catechins and dopamine, to produce novel fluorinated analogues.

Studies of the toxicological potential of capsinoids, XI: pharmacokinetic and tissue distribution study of 14C-dihydrocapsiate and metabolites in rats.

Pharmacokinetics of a single gavage dose of (14)C-labeled dihydrocapsiate (10 mg/kg) were investigated in male rats. Maximal plasma concentration was achieved in 40 minutes and exhibited an apparent half-life of 2.4 hours.

Disposition of low doses of 14C-bisphenol A in male, female, pregnant, fetal, and neonatal rats.

Bisphenol A (BPA) is a weak xenestrogen (ADI = 50 microg kg(-1), US EPA) which is mass-produced, with potential for human exposure. To study absorption, distribution, excretion, and metabolism of BPA, BPA labeled with carbon-14 was administered p.o.

Osteopontin-deficiency suppresses growth of B16 melanoma cells implanted in bone and osteoclastogenesis in co-cultures.

Unlabelled: Tumor metastasis and invasion to bone is one of major medical issues in our modern societies. Osteopontin deficiency decreased tumor invasion in bone based on knockout mouse study. In bone, osteopontin is a positive factor to increase tumor invasion.