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Distribution of KAI-9803, a Novel δ-Protein Kinase C Inhibitor, after Intravenous Administration to Rats
KAI-9803 is composed of a selective δ-protein kinase C (δPKC) inhibitor peptide derived from the δV1-1 portion of δPKC (termed “cargo peptide”), conjugated reversibly to the cell-penetrating peptideExpand
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Combination of GSH Trapping and Time-Dependent Inhibition Assays as a Predictive Method of Drugs Generating Highly Reactive Metabolites
Covalent binding (CB) of reactive metabolites (RMs) is potentially involved in severe adverse drug reactions. Because the CB assay is of low throughput and costly, a qualitative trapping assay usingExpand
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Use of an intravenous microdose of 14C-labeled drug and accelerator mass spectrometry to measure absolute oral bioavailability in dogs; cross-comparison of assay methods by accelerator mass
A technique utilizing simultaneous intravenous microdosing of (14)C-labeled drug with oral dosing of non-labeled drug for measurement of absolute bioavailability was evaluated using R-142086 in maleExpand
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Appearance of Double Peaks in Plasma Concentration–time Profile after Oral Administration Depends on Gastric Emptying Profile and Weight Function
PurposeMechanism for double-peak occurrence in plasma concentration profile after oral administration of drugs is controversial, although irregular gastric emptying would be an important factor. TheExpand
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Advantage of the Dissolution/Permeation System for Estimating Oral Absorption of Drug Candidates in the Drug Discovery Stage.
In order to increase the success rate in the development of oral drugs, an in vitro method, which can accurately estimate human oral absorption of a large variety of compounds from solidExpand
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Pharmacokinetics and disposition of recombinant human osteoprotegerin (rhOPG) after intravenous administration in female fischer rats
Osteoprotegerin (OPG) is a secreted member of the tumour necrosis factor receptor (TNFR) family that leads to the suppression of the differentiation, activation and survival of osteoclasts. TheExpand
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Novel Comb-Shaped PEG Modification Enhances the Osteoclastic Inhibitory Effect and Bone Delivery of Osteoprotegerin After Intravenous Administration in Ovariectomized Rats
PurposeRecombinant osteoprotegerin (OPG) has been proven to be useful for treating various bone disorders such as osteoporosis. To improve its in vivo pharmacological effect, OPG was conjugated toExpand
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Energy-saving Technology for Railway Traction Systems Using Onboard Storage Batteries
Motomi Shimada Yoshihiro Miyaji Takashi Kaneko Keita Suzuki OVERVIEW: The first application for onboard storage batteries came with the commercialization of series hybrid drive systems that reducedExpand
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Combination of glutathione trapping and time-dependent inhibition assays as a predictive method of drugs generating highly reactive metabolites
Drug Metabolism and Pharmacokinetics Research Laboratories (S.N., H.T., A.W., Y.M., W.S., D.S., T.I.), Daiichi Sankyo Co., Ltd., 1-2-58, Hiromachi, Shinagawa-ku, Tokyo, 140-8710, Japan Clinical DataExpand
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