Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter.

  title={Effects of 4-hydroxyantipyrine and its 4-O-sulfate on antipyrine as biodistribution promoter.},
  author={Y Ohkawa and M Matsumura and Yuji Kurosaki and Masateru Kurumi and Kenji Sasaki and Taiji Nakayama},
  journal={Biological \& pharmaceutical bulletin},
  volume={24 5},
The effects of 4-hydroxyantipyrine (4-OH), a major metabolite of antipyrine, and its 4-O-sulfate (4-S) on the pharmacokinetics of antipyrine were investigated in rats. Plasma elimination of intravenously administered antipyrine was significantly decelerated under a steady-state concentration of 4-OH but not under that of 4-S. Tissue-to-plasma concentration ratio (Kp) of antipyrine under its steady-state concentration was significantly increased in the brain and heart by the concomitant use of 4… 
Application of 4-hydroxyantipyrine and acetaminophen O-sulfate as biodistribution promoter.
The increment in the drug distribution to the brain with the concomitant use of 4-OH (or APAPS) observed in this study is useful information for the application of drug combinations as biodistribution promoters.
Kinetic Analysis of the Transport of Salicylic Acid, a Nonsteroidal Anti-inflammatory Drug, across Human Placenta
A pharmacokinetic model is developed, which should enable us to estimate the influx profile of drugs into umbilical arterial blood from the maternal plasma concentration profile.
Study on glutathionesulfonic acid sodium salt as biodistribution promoter for thiopental sodium.
The increment in the drug distribution to tissues with concomitant GSO3Na observed in this study is useful information for the application of drug combinations as a biodistribution promoter.
Direct determination of glucuronide and sulfate of p-hydroxymethamphetamine in methamphetamine users' urine.
The detection of sulfation in methamphetamine (MA) users' urine suggests that sulfation is a major pathway in the MA phase II metabolism.
Effects of endotoxin derived from Escherichia coli lipopolysaccharide on the pharmacokinetics of drugs
An attempt to explain changes in the pharmacokinetics of drugs reported in the literature was made in terms of hepatic CYP isozyme changes or urinary excretion changes in ECLPS rats.
Prediction and evaluation of fetal toxicity induced by NSAIDs using transplacental kinetic parameters obtained from human placental perfusion studies.
The results suggest that the fetal risk of diclofenac is higher than those of salicylic acid and antipyrine, and human placental perfusion study and pharmacokinetic/pharmacodynamic analysis may provide basic data for predicting human fetal toxicity of drugs.
Transplacental Pharmacokinetics of Diclofenac in Perfused Human Placenta
Human placental perfusion and transplantacental pharmacokinetic modeling allowed us to determine the transplacental transfer properties of diclofenac quantitatively and l-lactic acid was found to share transplACental transfer system(s) with l- lactic acid.
Prediction of sustained fetal toxicity induced by ketoprofen based on PK/PD analysis using human placental perfusion and rat toxicity data
The model with effect compartment and the obtained parameters predicted that use of multiple ketoprofen patches could potentially cause severe DA constriction in the human fetus, and that fetal toxicity might persist after ketopofen discontinuation by the mother, as observed in this case.
Characterization of Transplacental Transfer of Paroxetine in Perfused Human Placenta: Development of a Pharmacokinetic Model to Evaluate Tapered Dosing
The transplacental transfer of paroxetine in perfused human placenta was characterized, fitting a pharmacokinetic model to the results and applying the model and parameters to evaluate a tapered dosage regimen to avoid withdrawal syndromes in neonates after delivery.


Effect of aspirin on biotransformation of 14C-acetaminophen in rats.
Aspirin administered to rats concomitantly with 14C-acetaminophen caused a reduction in the rate but not in the extent of acetaminophen absorption from the GI tract and an enhanced blood level of radioactivity during the postabsorptive phase, irrespective of the route of administration.
Biopharmaceutical studies on drug/conjugated-metabolite interactions. III. Effect of acetaminophen sulfate and its positional isomers on the pharmacokinetics of acetaminophen in rats.
It was suggested that APAPS has not only the displacing activity of serum protein binding but also other specific effectiveness on the distribution of APAP.
Biopharmaceutical studies on drug/conjugated-metabolite interactions. II. Effect of acetaminophen sulfate on pharmacokinetics of acetaminophen in rats
The effect of conjugated-metabolite, acetaminophen sulfate (APAPS), on the pharmacokinetics of its parent drug, acetaimnophen (APAP), was examined in rats. Following the i.v. bolus administration of
Biopharmaceutical studies on drug/conjugated-metabolite interactions. I. Fate of acetaminophen sulfate, a major conjugated metabolite of acetaminophen, in rats
Abstract The plasma elimination kinetics and intestinal absorption kinetics of acetaminophen sulfate (APAPS), a major conjugated metabolite of acetaminophen (APAP), indispensable for the kinetic
Characterization of binding sites for sulfadimethoxine and its major metabolite, N4-acetylsulfadimethoxine, on human and rabbit serum albumin.
It can be presumed from the displacement data with a series of p-aminobenzoates that the characteristics of the binding sites (such as depth and width of the hydrophobic cleft) for SDM and N4-AcSDM on RSA may be almost the same, but the characteristicsOf these drug-binding sites on HSA may be somewhat different.
Pharmacokinetics of acetaminophen sulfate after oral administration in rats: analysis of plasma profiles exhibiting a non-linear second peak.
The pharmacokinetics of the two-peak plasma profiles of orally administered acetaminophen sulfate (APAPS) in rats was examined by a two-compartment model having two delivery routes: a direct delivery route of APAPS absorbed in an unchanged form and an indirect one where APAPS was absorbed as APAP after deconjugation in the lower intestine.
Putrescine‐Modified Nerve Growth Factor: Bioactivity, Plasma Pharmacokinetics, Blood‐Brain/Nerve Barrier Permeability, and Nervous System Biodistribution
The design of this polyamine‐modified NGF derivative that has enhanced permeability at the blood‐brain and blood‐nerve barriers with retained bioactivity may obviate the necessity to create small‐molecule mimics of NGF and may be applicable to neurotrophins, engineered multifunctional chimeric neurons, antioxidant enzymes, and other therapeutic proteins with specific clinical application to neurological diseases.
Transport of α-Aminoisobutyric Acid across Brain Capillary and Cellular Membranes
These studies indicated that the transport of AIB into brain cells was approximately 110 to 265 times greater than that across normal brain capillaries per unit mass of brain tissue, and that the BBB limits blood-to-brain cell transport of this amino acid.
Inhibition of brain choline uptake by isoarecolone and lobeline derivatives: implications for potential vector-mediated brain drug delivery
Delivery of certain compounds to brain is restricted by the nature of the blood-brain barrier (BBB). Many valuable pharmaceuticals are excluded from the CNS due to hydrophilicity or charge. These
Stress-Induced Increase in Blood–Brain Barrier Permeability in Control and Monosodium Glutamate-Treated Rats
It is concluded that short-lasting immobilization stress increased BBB permeability in some but not all brain regions studied, and BBB vulnerability in glutamate-treated rats during stress exposure was increased in the hypothalamus and decreased in the brain stem.