Minoru Akimoto

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1. Studies using human liver microsomes and recombinant human cytochrome P450 (CYP) and flavin-containing monooxygenase (FMO) were performed to identify the enzymes responsible for the metabolism of S-methyl-esonarimod (M2), an active metabolite of esonarimod (KE-298, a novel antirheumatic drug). 2. S-oxidative activities of M2 significantly correlated with(More)
In order to obtain an insight into the retention mechanism of drugs with imidazole moiety in the connective tissue, the in vitro characteristics of the interaction between 14C-labeled imidazoles (imidazole and its 2-methyl derivative) and slices of dog aorta were studied. We found that cupro-ascorbate-catalyzed oxidative reactions for the imidazoles led to(More)
Gastric pH levels were measured in samples of gastric aspirates from eight fasted beagle dogs. The gastric pH in fasting dogs fluctuated from 2.7 to 8.3, with a mean of 6.8+/-0.2 (SE). Each dog received the following four treatments in randomly-assigned order: (A) distilled water; (B) a placebo capsule; (C) pentagastrin, and (D) ranitidine. The gastric pH(More)
Pressure-length-diameter relationships of neonatal and adult rabbit ureters were studied in vitro. The increase in diameter, in response to an intraluminal pressure load of 10, 20, and 40 g per cm2, was faster and greater in the neonate than in the adult. Incubation in norepinephrine decreased the diametral deformation of neonatal ureters but had little(More)
To elucidate the retention mechanism of drugs with imidazole moiety in the connective tissue, the retention form and site of [2-14C]imidazole and 2-methyl[2-14C]imidazole were studied after intravenous administration to rats (3 micromol/kg body weight). The aorta, which is representative of the connective tissue, retained considerable radioactivity after(More)
2-Methylimidazole (2MI), as well as imidazole, has been thought to undergo cupro-ascorbate (Cu-VC)-catalyzed oxidative transformation in vitro to become a reactive species capable of combining with aldehydes intrinsic to connective-tissue proteins. We attempted to seize the essence of the above reaction through obtaining the structural information of an(More)
Isoforms of cytochrome P-450 (CYP) involved in the metabolism of gallopamil enantiomers were identified by measuring the disappearance rate of parent drug from an incubation mixture with human liver microsomes and recombinant human CYPs. Mean (+/- S.D.) intrinsic clearances (CL(int)) of R(+)- and S(-)-gallopamil in human liver microsomes were 0.320 +/-(More)
The immunohistochemical expression of DF3 antigen and serum concentrations of CA15-3, a breast carcinoma-associated antigen recognized by the monoclonal antibodies (MAbs) 115D8 and DF3, was investigated in breast cancer patients. The levels of serum CA15-3 in 23 primary breast cancer patients did not correlate to the percentage cytoplasmic reactivity of MAb(More)
A simultaneous analysis of the pharmacokinetics and pharmacodynamics of TS-943, a selective nonpeptide platelet glycoprotein-IIb/IIIa (GPIIb/IIIa) receptor antagonist, was made in dogs using a nonlinear mixed effect model. Plasma concentrations of TS-943 were determined after bolus intravenous injection, constant infusion and bolus plus constant infusion.(More)
The pharmacokinetics and pharmacodynamics of TS-943 were evaluated with use of NONMEM in 36 healthy male subjects after constant infusion of five different single-dose regimens. Population analysis showed the plasma concentration-time profiles of TS-943 to be best-fit characterized by a two-compartment open model with constant infusion and first-order(More)
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