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  • 1
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 27 (1984), S. 335-339 
    ISSN: 1432-1041
    Keywords: transdihydrolisuride ; dopamine agonist ; pharmacokinetics ; pharmacodynamics ; prolactin levels ; side-effects ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Plasma levels and urinary excretion of the dopamine agonist, transdihydrolisuride (TDHL), were measured by radioimmunoassay in healthy male volunteers given TDHL 50 µg i.v. and oral doses of 200, 400 and 800 µg. Plasma prolactin was also measured by radioimmunoassay. Following i.v. injection, the concentration of TDHL declined with a half-life of 37±19 min. The total clearance was 38±27 ml/min/kg and the apparent volume of distribution was 1.3±0.4 l/kg. The bioavailability of oral TDHL was proportional to the dose; after 200, 400 and 800 µg the bioavailability was 20±25%, 31±24% and 48±26%. TDHL was almost totally metabolized and less than 0.5% of the dose was excreted unchanged in urine in 24 h. Plasma prolactin levels were depressed by 66±15%, 75±11% and 80±7% after TDHL 200 µg, 400 µg and 800 µg. The effect lasted for more than 12 h after the lowest dose and for more than 24 h after 400 and 800 µg. Side effects, mainly nausea and headache, only occurred at the two highest dose levels.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-1041
    Keywords: lisuride ; prolactin ; plasma levels ; halflife ; pharmacokinetics ; dopamine agonist
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The development of a sensitive radioimmunoassay for the determination of lisuride in plasma is described. The antiserum against lisuride-4-hemisuccinate-BSA was raised in rabbits. Using this method the plasma levels of lisuride were monitored following one intravenous (25 µg) and two oral (100 µg and 300 µg) doses of lisuride hydrogen maleate in three female and three male volunteers (intraindividual comparison). The plasma prolactin was also determined by radioimmunoassay. Following i. v. injection, the concentration of lisuride declined in three phases, with half-lives of 5 min, 25 min and 2 h. The total plasma clearance of 800±250 ml × min−1 was in the range of “plasma flow” through the liver. In agreement with the high rate of biotransformation, the bioavailability of lisuride administered orally was 10%±7% of the 100-µg dose, and 22%±7% of the 300-µg dose. The plasma prolactin was lowered to 3%–18% of its pretreatment value depending on the route of administration and the dose. The reduction appeared to be short-lived and to be directly dependent on the plasma concentration of lisuride. Following intravenous injection, the prolactin level declined after a so far unexplained lagtime of 0.5 h.
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Journal of radioanalytical and nuclear chemistry 219 (1997), S. 61-67 
    ISSN: 1588-2780
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Energy, Environment Protection, Nuclear Power Engineering
    Notes: Abstract The extractive properties of tri-isoamyl-phosphate (TAP), an indigenously prepared extractant, and the loading capacity of extraction solvent containing TAP for U(VI) and Pu(IV) ions in nitric solution have been investigated. The dependence of the distribution ratio on the concentration of nitric acid showed that TAP has an ability to extract these actinides, while the fission product contaminants are poorly extracted. The distribution data revealed a quantitative extraction of both U(VI) and Pu(IV) from moderate nitric acidities in the range 2–7 mol · dm−3. Slope analysis proved predominant formation of the disolvated organic phase complex of the type UO2(NO3). 2TAP and Pu(NO3)4·2TAP with U(VI) and PU(IV), respectively. On the contrary, the extraction of fission product contaminants such as144Ce,137Cs,9Nb.,147Pr,106Ru,95Zr was almost negligible even at very high nitric acid concentrations in the aqueous phase indicating its potential application in actinide partitioning. The recovery of TAP from the loaded actinides could be easily accomplished by using a dilute sodium carbonate solution or acidified distiled water (≈0.01 mol · dm−3 HNO3) as the strippant for U(VI) and using uranous nitrate or ferrous sulphamate as that for Pu(IV). Radiation stability of TAP was adequate for most of the process applications.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-0878
    Keywords: Cyproterone acetate ; 17β-Oestradiol ; 5α-Androstane-3α,17β-diol ; Prostate gland ; Pituitary gland ; Immunocytochemistry ; Dog (beagle)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary The antiandrogen, cyproterone acetate (CPA), prevents development of prostatic hyperplasia, induced in castrated dogs by a 6 month-treatment with 5α-androstane-3α,l 7β-diol (A)alone or in combination with 17β-oestradiol (E 2). The immunoperoxidase technique was used to study functional cell types in the pars distalis of the pituitary gland and to detect growth hormone (GH) and prolactin (PRL) target sites in the prostate gland. Homologous radioimmunoassays for estimation of serum canine GH and PRL concentrations were also performed. Treatment with the combinations A + E 2 and A + E 2 + CPA resulted in morphological indications of stimulated GH and PRL cells and depressed gonadotrophs. This correlates well with an increase in PRL-dependent staining in glandular epithelium and fibromuscular tissue of the prostate gland. However, basal serum PRL and GH levels were not significantly affected. Treatment with A and A + E2 stimulated, while additional treatment with CPA clearly suppressed adrenocorticotrophin/melanotrophin (ACTH/MSH) cells. These findings indicate that an endocrine imbalance in hypothalamic-pituitary-adrenal function may be involved in induction and prevention of prostatic hyperplasia in the dog.
    Type of Medium: Electronic Resource
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