Abstract：
:The effects of aluminium, manganese, ferrous and ferric iron, cobalt, nickel, copper, zinc, cadmium, barium, mercury and lead ions on the rat hepatic UDPglucuronosyltransferase activity with regard to 4-methylumbelliferone, 4-nitrophenol, bilirubin, and 2-aminophenol were investigated in vitro. Conjugation of bilirubin was found to be activated by manganese, cobalt, nickel, cadmium, mercury and lead ions in native microsomes, but not in digitonin-treated microsomes. Aluminum, ferrous iron, cadmium, barium and lead increased the conjugation of 4-nitrophenol in native microsomes and aluminium in digitonin-treated microsomes as well. Lead slightly activated 4-methylumbelliferone conjugation, whereas none of the metal salts studied were found to activate the conjugation of 2-aminophenol. Copper and zinc salts inhibited all conjugations. In digitonin-treated microsomes, the conjugation of 4-nitrophenol was inhibited by cadmium and mercury, that of 4-methylumbelliferone by nickel and lead as well. The sensitivity of 4-methylumbelliferone conjugation to inhibition by mercury was most pronounced in microsomes prepared from rats pretreated with 2,3,7,8-tetrachlorodibenzo-p-dioxin.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Aitio A,Ahotupa M,Parkki MGdoi
10.1007/BF03189441subject
Has Abstractpub_date
1980-01-01 00:00:00pages
35-40issue
1eissn
0378-7966issn
2107-0180journal_volume
5pub_type
杂志文章abstract：BACKGROUND AND OBJECTIVES:Clopidogrel is an antiplatelet and antithrombotic prodrug. It has poor oral bioavailability due to poor dissolution and possible premature degradation in the intestine. Accordingly, the objective of this study was to enhance clopidogrel dissolution rate and to reduce its premature degradation ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-015-0311-4
更新日期：2016-12-01 00:00:00
abstract：:The pharmacokinetics of tolbutamide (TB) have been studied in endotoxin pretreated rats with the aim of evaluating TB as a marker for endotoxin effects. Endotoxin dose of 10 mg/kg resulted in a 50% rate of mortality. TB was i.v. administered 24 h. after endotoxin dosing. Clearance (Cl) decreased by approximately 2/3 o...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190205
更新日期：1990-07-01 00:00:00
abstract：:The hypoxic cell radiosensitizing drug, misonidazole (Miso) (Ro 07-0582) and its demethylated metabolite were administered to Wistar rats at different dose levels to examine their renal elimination. The data were consistent with a model in which Miso is eliminated mainly after biotransformation into desmethylmisonidaz...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189740
更新日期：1985-07-01 00:00:00
abstract：:Carboxylesterases (CESs) play major roles in catalyzing the hydrolysis of a wide range of ester- and amide-containing compounds. CESs dominate both the biotransformation of numerous therapeutic drugs and the detoxification of environmental toxicants, and the activity alteration of CESs may be a determinant reason for ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,评审
doi：10.1007/s13318-016-0326-5
更新日期：2016-08-01 00:00:00
abstract：BACKGROUND:MTBH, a novel hesperetin derivative, possesses in vivo hepatoprotective effects against carbon tetrachloride (CCl4)-induced acute liver injury in Institute of Cancer Research (ICR) mice. OBJECTIVES:This study investigated the pharmacokinetics and tissue distribution of MTBH and its conjugated metabolites in...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-015-0293-2
更新日期：2016-12-01 00:00:00
abstract：:We studied the pharmacokinetics of moguisteine, a racemic non-narcotic peripheral antitussive drug, in 12 healthy male subjects after a single oral administration of 200 mg. The unchanged drug was absent in plasma and urine of all subjects. Moguisteine was immediately and completely hydrolyzed to its main active metab...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190242
更新日期：1995-10-01 00:00:00
abstract：:Hyaluronic acid (HA), is a high molecular weight (HMW) glucosaminoglycan with significant acitivity, and which influences a number of physiological and pathological processes such as tumorogenesis, arthritis, etc. The aim of this study was to determine the difference in the biodistributional pathways of 111In-labeled ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03191112
更新日期：2008-07-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:A clinical trial was conducted to measure and analyse the pharmacokinetic parameters of a lipid formulation of risperidone, VAL401. The VAL401 formulation is designed to repurpose risperidone from an antipsychotic to an adenocarcinoma treatment, with the lipid formulation altering the cellular...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-018-00538-4
更新日期：2019-08-01 00:00:00
abstract：:The cardioselective beta-adrenergic blocking drug Visacor (ICI 141,292) was dosed to six beagle dogs in a randomized cross-over manner. Five formulations were examined i.e. a 15 mg/kg intravenous solution, a 50 mg/kg oral solution, and 50, 100 and 200 mg/kg oral powder formulations. Whole blood and urine samples were ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189616
更新日期：1984-04-01 00:00:00
abstract：:Blood loss during cesarean section was calculated based on post-operative decrement of hemoglobin (Hb) and hematocrit (Hct) level. The model used for pregnant women was previously validated for non-pregnant women who underwent gynecological surgery. 1,068 pregnant women who underwent cesarean section and 517 women who...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-011-0042-0
更新日期：2011-09-01 00:00:00
abstract：:The kinetics of the nootropic drug oxiracetam was studied in 6 elderly female patients (age range 69-96 years) in good physical condition. After a single oral dose (800 mg), serum oxiracetam levels reached a peak (25 +/- 6 micrograms/ml) within 1-3 h and declined thereafter with a half-life of 3 to 6 h. Eighty-four pe...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189889
更新日期：1987-04-01 00:00:00
abstract：:Sertraline potently inhibits cytochrome P450 2B6 (CYP2B6) in vitro. Bupropion is commonly co-prescribed with sertraline and is exclusively metabolized by CYP2B6 to its major active metabolite hydroxybupropion. Putatively the co-administration of bupropion and sertraline could lead to a significant pharmacokinetic drug...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-011-0065-6
更新日期：2012-03-01 00:00:00
abstract：:A single oral dose of 300 mg of nizatidine was administered to two groups of volunteers: a first group of 12 young healthy subjects and a second group of 12 elderly patients, in order to compare the pharmacokinetic parameters and to verify a possible influence of the age on nizatidine's kinetics. Blood samples were co...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：
更新日期：1991-01-01 00:00:00
abstract：:The compound 4-amino-3-(3'-methoxycarbonyl-2'-thioureido) benzophenone has shown promise as a prodrug of the anthelmintic mebendazole. The compound is stable in acid and neutral media and is rapidly hydrolysed in base. An HPLC assay procedure for mebendazole, the prodrug and their known or expected metabolites and deg...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03188765
更新日期：1983-10-01 00:00:00
abstract：:Vitexin-4″-O-glucoside (VOG), being a main component in the leaves of Crataegus pinnatifida Bge. var. major, was isolated and then three different doses (20, 40, and 60 mg/kg) of VOG were administered intravenously to rats. To study its pharmacokinetics, a simple and rapid HPLC method was developed using hesperidin as...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-011-0071-8
更新日期：2012-06-01 00:00:00
abstract：:Apomorphine was administered subcutaneously and intranasally to 7 patients suffering from Parkinsonism with 'on-off' problems. This comparative pharmacokinetic study showed that the two routes of administration are comparable with respect to absorption kinetics. Apomorphine is rapidly absorbed when administered intran...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章
doi：10.1007/BF03192285
更新日期：1995-01-01 00:00:00
abstract：:Currently, macromolecular drugs such as proteins are mainly administered by means of injections due to their low intestinal epithelial permeability and poor stability in the gastrointestinal tract. This study investigated binary combinations of chemical drug absorption enhancers to determine if synergistic drug absorp...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-015-0280-7
更新日期：2016-10-01 00:00:00
abstract：:Cytochrome P450 from rat brain mitochondrial and microsomal fractions was found to be inducible by 3-methylcholanthrene, both in quantity of enzyme and in activity towards 7-ethoxyresorufin, which is a model substrate for the cytochrome P450 isoform specifically induced by 3-methylcholanthrene. Conversely, a phenobarb...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189910
更新日期：1987-10-01 00:00:00
abstract：:The present study reports findings on the disposition of epirubicin after an intrahepato-arterial administration of the Lipiodol-drug complex, prepared by mixing the drug-aqueous phase with the iodized oil by ultra-sonification, in 14 patients with histologically proven hepatoma or hepatomegaly with serum alpha-fetopr...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190149
更新日期：1992-07-01 00:00:00
abstract：:Because of its special pharmacokinetic properties, plasma levels of theophylline show significant differences between individuals and also its therapeutic index is very low. So, plasma theophylline concentration measurements are essential for an effective and safe treatment. In the present study, age related differenc...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 临床试验,杂志文章,随机对照试验
doi：10.1007/BF03188821
更新日期：1994-01-01 00:00:00
abstract：BACKGROUND:Aldehyde oxidase (AOX) is an important molybdenum-containing enzyme with high similarity with xanthine oxidase (XO). AOX involved in the metabolism of a large array of aldehydes and N-heterocyclic compounds and its activity is highly substrate-dependent. OBJECTIVES:The aim of this work was to study the effe...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-018-0514-6
更新日期：2019-04-01 00:00:00
abstract：:Hepatic transporters and metabolic enzymes affect drug pharmacokinetics. Limited information exists on the alteration in mRNA levels of hepatic transporters and metabolic enzymes with aging. We examined the effects of aging on the mRNA levels of representative hepatic drug transporters and metabolic enzymes by analyzi...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-014-0208-7
更新日期：2015-06-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Hydronidone is a novel pyridine derivative with therapeutic potential for hepatic fibrosis. The aim of this study was to investigate the safety, tolerability, and pharmacokinetics of hydronidone in healthy subjects. Effects of sex and food on hydronidone pharmacokinetics were also evaluated. ...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章,随机对照试验
doi：10.1007/s13318-015-0316-z
更新日期：2017-02-01 00:00:00
abstract：BACKGROUND AND OBJECTIVES:Maximum plasma concentration of biopharmaceuticals sometimes occurs long after completion of intravenous infusion. The objective of this research was to study the hypothetical adsorption of biopharmaceuticals to endothelium and infusion material, which may theoretically explain this phenomenon...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-017-0430-1
更新日期：2018-02-01 00:00:00
abstract：:The disposition of a single 80 mg/kg injection of quinine base was compared in control and Plasmodium berghei-infected mice. Pharmacokinetic parameters were determined on repeated whole blood samples from caudal vein (experiment 1) and quinine distribution was evaluated in tissues and blood fractions from mice sacrifi...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190862
更新日期：2003-01-01 00:00:00
abstract：:We have studied the metabolism of doxorubicin in rat and mouse liver, heart and hepatocytes. Doxorubicinol was present in all cases at very low levels and 7-deoxyaglycones were present only in extraphysiological conditions: no aglycones were found either in fresh livers or in hearts of animals treated with the drug, b...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03189834
更新日期：1986-04-01 00:00:00
abstract：:This study examined the effects of the absorption enhancers, acylcarnitines, on efflux transporting systems, including P-glycoprotein (P-gp) and other efflux transporters, and elucidated the importance of acyl chain length and the concentration of acylcarnitine on the activity of efflux transport. The effects of two a...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-010-0001-1
更新日期：2010-09-01 00:00:00
abstract：:The technique of differential display reverse transcription-polymerase chain reaction (ddRT-PCR) has been used to produce unique profiles of up-regulated and down-regulated gene expression in the liver of male Wistar rats following short term exposure to the non-genotoxic hepatocarcinogens, phenobarbital and WY-14,643...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190966
更新日期：1997-10-01 00:00:00
abstract：:Changes in liver perfusion may have a substantial influence on the pharmacokinetics of drugs with flow-controlled metabolism. This may have important implications for drug dosage in patients in an intensive care unit (ICU). The hepatic D-sorbitol plasma clearance has been suggested as a non-invasive test for evaluatin...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/BF03190181
更新日期：1993-10-01 00:00:00
abstract：:The main objective of this study was to investigate the release and pharmacokinetic profiles of ketoprofen (KP) from developed thermosensitive and mucoadhesive liquid suppositories. Thermosensitive liquid suppositories were prepared using KP, poloxamer 407 (P 407), poloxamer 188 (P 188) and various amounts of differen...
journal_title：European journal of drug metabolism and pharmacokinetics
pub_type： 杂志文章
doi：10.1007/s13318-013-0157-6
更新日期：2014-12-01 00:00:00
