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  • 1
    Electronic Resource
    Electronic Resource
    Valpromide is a poor inhibitor of the cytosolic epoxide hydrolase (1989)
    Springer
    Archives of toxicology 63 (1989), S. 157-159 
    Details
    ISSN: 1432-0738
    Keywords: Cytosolic epoxide hydrolase ; Valpromide ; Liver ; Adult subjects and fetuses
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effect of the antiepileptics valpromide and sodium valproate on the cytosolic epoxide hydrolase was studied in human fetal liver, kidneys and adrenals and from human adult liver and kidneys. Trans-stilbene oxide was used as substrate. Valpromide (10 mM) lowered the activity of the epoxide hydrolase to one half of the control in all organs studied. Sodium valproate (10 mM) was less powerful as an inhibitor than valpromide; however, it exerted a significant inhibition in all tissues studied.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00316440
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  • 2
    Electronic Resource
    Electronic Resource
    Sulphation of the heterocyclic amine 1,2,3,4-tetrahydroisoquinoline in the human liver and intestinal mucosa: interindividual variability (1997)
    Springer
    Archives of toxicology 71 (1997), S. 477-481 
    Details
    ISSN: 1432-0738
    Keywords: Key words Sulphotransferase ; Liver ; Intestine ; Man ; Variability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The sulphation rate of 1,2,3,4-tetrahydroisoquinoline (TIQ) was measured in the human liver and in the intestinal mucosa isolated from the transverse colon, ileum and duodenum. The rate (mean ± SD) of hepatic TIQ sulphation was 500 ± 174 pmol/min per mg in women (n=61) and 591 ± 201 in men (n=39; P=0.0087), varying over one order of magnitude in men and women. The sulphation rate of testosterone showed the same sex-dependent pattern and was correlated (r=0.6055; P〈0.001) with that of TIQ. The frequency distribution of TIQ sulphation rate in human liver was bimodal: 70% of the population fell into the low-activity subgroup and the remaining 30% feel into the high-activity subgroup. In the colon (n=56), the rate of TIQ sulphation was 30.4 ± 15.6 pmol/min per mg and the values were similar in men and women (29.8 and 30.9 pmol/min per mg, respectively) but, varied over one order of magnitude and correlated (r=0.7231; P〈0.001) with that of 4-nitrophenol. The rate of TIQ sulphation changed along the human bowel and mean (±SD) estimates for duodenum, ileum and transverse colon were 444 ± 25, 182 ± 87  and 30.4 ± 15.6 pmol/min per mg, respectively. The present results are consistent with the view that the heterocyclic amine TIQ is sulphated in the human liver and intestinal mucosa. TIQ-sulphotransferase activity varies among subjects and is mostly associated with the liver and duodenum.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/s002040050415
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  • 3
    Electronic Resource
    Electronic Resource
    Hydroxylation of dibutylnitrosamine in the human liver and intestinal microsomal fractions (1986)
    Springer
    Archives of toxicology 58 (1986), S. 196-198 
    Details
    ISSN: 1432-0738
    Keywords: Dibutylnitrosamine ; Metabolism ; Human ; Rat ; Liver ; intestine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The metabolism of the bladder carcinogen N-nitroso-di-n-butylamine (NDBA) was studied in microsomal preparations of tissues of patients of both sexes, aged 59–69 years undergoing abdominal surgery. Samples of liver, ileum, and colon were of normal histological appearance. For comparison, samples of rat liver and small intestinal mucosa microsomes were included in the study. Using 1-14C-labeled NDBA, the biotransformation to hydroxylation products retaining the nitroso group, NDBA-2-OH, NDBA-3-OH, and NDBA-4-OH, respectively, was investigated by reversed phase HPLC. In order to separate these metabolites, pooled samples were analysed by normal phase HPLC. The rate of hydroxylation of NDBA was found to be 5.5 times higher in rat liver microsomes compared to those from human liver (2.86±0.29 vs 0.52±0.03 nM x min−1 x mg−1). NDBA-3-OH proved to be the major metabolite formed (〉80% of total metabolites). The metabolism of NDBA was low but detectable in seven out of nine specimens of human gut, 0.1–0.5 nM x mg−1 in 1 h of incubation, and of the same order of magnitude in rat intestinal tissue (0.4–0.6 nM x mg−1).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00340981
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  • 4
    Electronic Resource
    Electronic Resource
    Cytosolic epoxide hydrolase in humans: development and tissue distribution (1988)
    Springer
    Archives of toxicology 62 (1988), S. 254-257 
    Details
    ISSN: 1432-0738
    Keywords: Cytosolic epoxide hydrolase ; Humans ; Fetuses ; Adult subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract Cytosolic epoxide hydrolase activity was measured towards trans-stilbene oxide in 41 human adult livers, in 40 fetal livers, in 17 placentas and in fetal and adult lungs, kidneys and gut. The cytosolic epoxide hydrolase activity was measurable in all specimens investigated. The rate of formation of trans-stilbene glycol (pmol/min per mg protein, mean±SD) was 55.2±89.6 (fetal liver). 303.2±73.2 (adult liver) and 18.8±13.1 (placenta) In the fetal extrahepatic tissues, the cytosolic epoxide hydrolase activity was 70.0±9.4 (adrenals), 47.6±7.2 (gut), 69.4±22.5 (kidneys) and 43.2±19.2 (lungs) pmol/min per mg protein, whereas in the adult tissues it was 131.2±63.1 (kidneys), 27.8±20.3 (intestine), 8.5±2.8 (lungs) and 7.2±4.2 (urinary bladder) pmol/min per mg protein.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00332483
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  • 5
    Electronic Resource
    Electronic Resource
    Morphine glucuronidation in human fetal and adult liver (1982)
    Springer
    European journal of clinical pharmacology 22 (1982), S. 553-558 
    Details
    ISSN: 1432-1041
    Keywords: glucuronidation ; morphine ; UDP-glucuronyltransferase ; adult liver ; fetal liver ; enzyme heterogeneity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The glucuronyltransferase activity towards morphine was measured in microsomes isolated from liver specimens obtained from human fetuses and cancer patients. All the fetal livers investigated had measurable UDP-glucuronyltransferase activity towards morphine. There was no correlation between the gestational age (15 to 27 weeks) and the glucuronidation rate. The mean value of the enzymatic activities was higher in fetal livers obtained by hysterotomy (0.20 nmoles×min−1×mg−1) than in livers obtained after induced abortion (0.11 nmoles×min−1×mg−1). The average rate of glucuronidation in microsomes from adult liver (mean 1.15 nmoles×mint-1×mg−1) was 6 to 10 times higher than in the fetal liver microsomes. Together with previous investigations on human adult and fetal liver glucuronidation, the present results support the theory of heterogeneity of human UDP-glucuronyltransferase.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00609630
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  • 6
    Electronic Resource
    Electronic Resource
    Presence of epoxide hydrolase and glutathione S-transferase in human pulmonary alveolar macrophages (1988)
    Springer
    European journal of clinical pharmacology 34 (1988), S. 419-421 
    Details
    ISSN: 1432-1041
    Keywords: epoxide hydrolase ; glutathione S-transferase ; pulmonary macrophages ; bronchoalveolar lavage ; smokers/non-smokers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Pulmonary alveolar macrophages (PAMs) were obtained from 11 patients by bronchoalveolar lavage. Epoxide hydrolase and glutathione S-transferase in sonicated PAMs were measured using benzo(a)pyrene-4,5-oxide as the substrate. The activity of epoxide hydrolase was 0.24±0.10 nmol/min/mg protein (mean±SD), and of glutathione S-transferase 0.22±0.12 nmol/min/mg protein. There was a significant difference in enzyme activities in the PAMs from smokers and non-smokers. Epoxides may be metabolized in PAMs.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00542447
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  • 7
    Electronic Resource
    Electronic Resource
    Distribution of 2-naphthol sulphotransferase and its endogenous substrate adenosine 3′-phosphate 5′-phosphosulphate in human tissues (1989)
    Springer
    European journal of clinical pharmacology 37 (1989), S. 317-320 
    Details
    ISSN: 1432-1041
    Keywords: 2-naphthol sulphotransferase ; adenosine 3′-phosphate 5′-phosphosulfate ; liver ; kidney ; lung ; intestine ; tissue distribution
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The activity of sulphotransferase towards 2-naphthol and the concentration of its endogenous substrate, adenosine 3′-phosphate 5′-phosphosulphate (PAPS), have been measured in five specimens of human liver, lung, and kidney, and the mucosa from the ileum and the ascending, descending and sigmoid colon. The activity of 2-naphthol sulphotransferase (mean nmol·min−1·mg−1 protein) was 1.82 (liver); 0.034 (kidney); 0.19 (lung); 0.64 (ileum); 0.47 (ascending colon); 0.50 (descending colon); 0.40 (sigmoid colon). The concentration of PAPS (mean nmol·g−1 wet tissue) was 22.6 (liver); 4.8 (kidney); 4.3 (lung); 12.8 (ileum); 8.1 (ascending colon); 7.5 (descending colon); 6.2 (sigmoid colon). The concentration of PAPS and the activity of 2-naphthol sulphotransferase were higher in the liver than in the extrahepatic tissues. There was significant difference between ileum and ascending colon, both the activity of sulphotransferase and the concentration of PAPS being higher in the former. 2-Naphthol sulphotransferase activity and the concentration of PAPS have consistent distribution patterns. Differences between the tissues studied were more marked for sulphotransferase than for its endogenous substrate.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00679793
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  • 8
    Electronic Resource
    Electronic Resource
    Pinazepam: A precursor of N-desmethyldiazepam (1982)
    Springer
    European journal of clinical pharmacology 22 (1982), S. 225-228 
    Details
    ISSN: 1432-1041
    Keywords: pinazepam ; N-desmethyldiazepam ; kinetics ; metabolism ; human
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma profile of a single oral dose of pinazepam 10 mg was studied in 6 healthy male volunteers, aged 26 to 31 years. The concentrations of the parent compound and of its metabolite in plasma were measured by gas-chromatography. The peak plasma levels of pinazepam was 36.8±5.1 ng/ml and of N-desmethyldiazepam 150±13.3 ng/ml. The plasma concentration of the metabolite become higher than that of the parent compound shortly after administration, suggesting that pinazepam acts as a prodrug.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00545219
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  • 9
    Electronic Resource
    Electronic Resource
    Interindividual variability in the rate of salbutamol sulphation in the human lung (1996)
    Springer
    European journal of clinical pharmacology 49 (1996), S. 299-303 
    Details
    ISSN: 1432-1041
    Keywords: Salbutamol ; lung ; sulphotransferase ; variability ; chirality
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The β2-adrenergic agonist salbutamol is administered by inhalation to treat lung-obstructive disease. Salbutamol is metabolized by conjugation with sulphate, and the sulphation of salbutamol was investigated in human lung. Specimens of lung were obtained at lobectomy from 11 non-smokers, 39 smokers and 46 ex-smokers, the latter refraining from smoking at least 6 months before surgery. Neither sex nor ageing influenced the activity of sulphotransferase. The rate of salbutamol sulphation (pmol·min-1·mg-1) was greater in non-smokers (27.7) than in smokers (21.3), whereas it was similar in smoker and ex-smokers (22.8). The rate of salbutamol sulphation ranged up to six fold and its distribution did not deviate from normality. As the rate of formation of the inactive salbutamol sulphate varied in the lung, the availability of salbutamol and, in turn, the evoked pharmacological effect should vary in parallel. The activities of salbutamol and dopamine sulphotransferase correlated, suggesting that catechol sulphotransferase takes part in the sulphation of salbutamol. The sulphation of salbutamol is stereoselective in the human lung, the k M estimate for (+)-salbutamol (1198 μM) being greater than those for either (-)-salbutamol (190 μM) and racemic salbutamol (142 μM). These results are consistent with the view that (-)-salbutamol is a better substrate than (+)-salbutamol for sulphotransferase.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00226331
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  • 10
    Electronic Resource
    Electronic Resource
    Minoxidil sulphation in human liver and platelets (1993)
    Springer
    European journal of clinical pharmacology 45 (1993), S. 337-341 
    Details
    ISSN: 1432-1041
    Keywords: Minoxidil ; sulphotransferase ; liver ; extrahepatic tissues ; platelets ; interindividual variability ; adults ; neonates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Minoxidil requires to be sulphated to exert its hypotensive effect. We report on interindividual variability in the rate of minoxidil sulphation in 118 specimens of human liver and in platelets obtained from 100 healthy subjects and 100 newborns. The frequency distribution histogram of the hepatic activity of minoxidil sulphotransferase was positively skewed; the mean was 631 pmol · min−1 · mg−1. After logarithmic transformation of the enzyme activity, the frequency distribution histogram became symmetrical and did not significantly deviate from normality. The rate of minoxidil sulphation was not different in platelets from adults (0.74 pmol · min−1 · mg−1) and newborns (1.16 pmol · min−1 · mg−1). The frequency distribution histograms were positively skewed and the results of normal equivalent deviation analysis was compatible with the presence of at least two subgroups of sulphotransferase in liver and platelets. Thus, two phenotypes of sulphotransferase exist in human liver and platelets, and the “extensive sulphator” phenotype contributes to skewing the frequency distribution. In platelets, the percentage of subjects that fall in the two subgroups is different at birth and in adulthood. This can explain the different shape of the frequency distribution in newborn and adult platelets and suggests that platelet minoxidil sulphotransferase undergoes modification after birth.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00265951
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