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  • 1
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    International journal of urology 4 (1997), S. 0 
    ISSN: 1442-2042
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: Background The effect of an artificial testicular prosthesis on sexual disturbance in hypogonadal men was investigated. Methods Twelve hypogonadal men were treated with testosterone replacement therapy delivered via radiation-polymerized testicular prostheses surgically implanted in their scrotums. Results An average serum testosterone level of over 200ng/dl was maintained for 48 months. Most patients treated with this prosthesis were satisfied with the improvement of their sexual activity. Moreover, the patients were psychologically more satisfied with the enlarged scrotum achieved with the implanted prosthesis. Conclusion We recommend this prosthesis as the first choice among testosterone-replacement therapies for hypogonadal men.
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Clinical and experimental pharmacology and physiology 22 (1995), S. 0 
    ISSN: 1440-1681
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 1. The effects of barnidipine on blood flow to major organs and on renal function were investigated in anaesthetized dogs and conscious spontaneously hypertensive rats (SHR), and the results were compared with those for nicardipine, nitrendipine, nisoldipine, manidipine and amlodipine.2. In anaesthetized dogs, barnidipine (0.3–3 μg/kg i.v.) dose-dependently decreased blood pressure and increased or preserved blood flow in the vertebral, coronary, femoral and renal arteries. The effect of barnidipine on blood flow was the most potent of the compounds tested. In conscious SHR, barnidipine (0.3–3 mg/kg p.o.) produced a dose-dependent antihypertensive effect and decreased renal vascular resistance. Barnidipine also dose-dependently increased urinary volume. The antihypertensive and diuretic effects of barnidipine were the most potent of the drugs tested.3. In summary, barnidipine was shown to preserve or increase blood flow to major organs and to produce diuretic activity with a decrease in blood pressure. These findings suggest that barnidipine maintains or promotes renal function at antihypertensive doses.
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  • 3
    ISSN: 1440-1681
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Medicine
    Notes: 1. Specific binding of [3H]-prazosin in prostatic and aortic membranes of humans was saturable and of high affinity (prostate: apparent dissociation constant, Kd= 0.35 ± 0.03 nmol/L; aorta: Kd= 0.26 ± 0.03 nmol/L). The density of [3H]-prazosin binding sites (Bmax) for prostate and aorta was 546 ± 31 and 61.6 ± 1.6 fmol/mg protein, respectively.2. Prazosin, YM617, naftopidil and urapidil competed with [3H]-prazosin for the binding sites in a dose-dependent manner in the prostate and aorta of humans. The binding affinities of these antagonists in both tissues were compared, based on the inhibition constant, Ki. Both prazosin and urapidil showed similar affinity to [3H]-prazosin binding sites in human tissue, whereas YM617 and naftopidil showed approximately a 12 and two times higher affinity, respectively, to α1-adrenoceptor sites of prostate than aorta.3. The chloroethylclonidine treatment reduced partially the Bmax values for specific [3H]-prazosin binding in the prostate and aorta of humans with little effect on the Kd values.4. These data suggest that YM617 is a relatively selective antagonist of human prostatic α1-adrenoceptors.
    Type of Medium: Electronic Resource
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  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 355 (1997), S. 203-209 
    ISSN: 1432-1912
    Keywords: Key words KATP channel opener ; PAF-induced airway hyperresponsiveness ; Guinea-pigs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effect of YM934 (2-(3,4-dihydro-2,2-dimethyl-6-nitro-2H-1,4-benzoxazin-4-yl)pyridine N-oxide) on airway hyperresponsiveness induced by platelet activating factor (PAF) was investigated in anesthetized guinea-pigs. Bronchoconstrictor responses to histamine were enhanced by intravenous (i.v.) infusion of PAF (600ng/kg/h for 1h). The KATP channel opener, YM934 (10–100μg/kg), given by i.v. bolus injection or i.v. infusion (75min) dose-dependently inhibited this PAF-induced airway hyperresponsiveness. In the normal control group, i.v. bolus injection of YM934 dose-dependently reduced the bronchoconstrictor responses to histamine. However, i.v. infusion of YM934 (100μg/kg) had almost no effect on responsiveness. Pretreatment with capsaicin (50mg/kg, s.c.), a depleter of neuropeptides, partially prevented the development of PAF-induced airway hyperresponsiveness. In contrast, phosphoramidon (2.5mg/kg, i.v.), an inhibitor of neutral endopeptidase, enhanced the airway hyperresponsiveness induced by PAF. Furthermore, YM934 inhibited PAF-induced airway hyperresponsiveness in guinea-pigs pretreated with capsaicin or phosphoramidon. The present results suggest that YM934 given by i.v. infusion reduces PAF-induced airway hyperresponsiveness at doses insufficient to produce a bronchodilatory effect. Further, the mechanism of YM934‘s inhibitory effect on airway hyperresponsiveness may involve bronchodilatory and other unidentified effects, such as a decrease in the release of neuropeptides from sensory nerve terminals.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: A homopolymer of L-lactic acid (LA), which was synthesized by direct polycondensation in the absence of a catalyst at 200°C, is crystalline, in contrast to the homopolymer of D,L-mandelic acid (MA) which is amorphous. Poly(LA-co-MA), obtained under the above conditions, is amorphous over a wide range of composition from 15 to 100 mol-% of monomeric units of MA. The in vitro degradation mechanism of these homopolymers shows a parabola-type degradation pattern for poly(LA) and no degradation throughout an experimental period of 15 weeks for poly(MA). In poly(LA-co-MA) the degradation mechanism leads to a typical S-type degradation pattern, which may be divided into two processes, initial swelling at the surface of the matrix without degradation (induction period), followed by the erosion of oligomers produced by degradation of the main chain in the swollen state.
    Additional Material: 6 Ill.
    Type of Medium: Electronic Resource
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  • 6
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: Degradable copolymers which respond to external stimuli such as pH, ionic strength, and temperature were successfully prepared by direct polycondensation of L-lactic acid (LA), D,L-mandelic acid (MA), and 3-(p-hydroxyphenyl)propionic acid (HPPA) without the use of a catalyst at 200°C by bubbling nitrogen through the solution. The molecular weights of the copolymers obtained were relatively low because of the low polymerizability of MA and HPPA, e. g., number-average molecular weight M̄n ≦ 2100 and weight-average molecular weight M̄w ≦ 4100. Poly{(L-lactic acid)-co-(D,L-mandelic acid)-co-[3-(p-hydroxyphenyl)propionic acid]} (poly(LA/MA/HPPA)) with a composition of the monomeric units (in mol-%) LA:MA:HPPA = 80:10:10 showed rapid degradation after a lag time of 5 h within 48 h from the start of the test, in M/15 phosphate buffer solution (pH 7,2) at 37°C. With increasing pH and temperature, the rate of degradation was markedly accelerated.
    Additional Material: 7 Ill.
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  • 7
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: The random copolypeptides of β-benzyl L-aspartate (β-Bz L-Asp) and γ-methyl L-glutamate (γ-Me L-Glu) were synthesized and implanted subcutaneously in rats. It was found that the resulting copolypeptides are degraded and also have good biocompatibility in vivo. On the basis of these results, poly(β-Bz L-Asp-co-γ-Me L-Glu) was tried to be used as a material for a drug delivery system. Copolypeptide-testosterone composites were prepared at a pressure of 200 kg/cm2 in the presence of a slight amount of dichloroethane. The in vivo release rate of testosterone from copolypeptide-drug composites was about 5,5 times higher than that in vitro. The in vivo release rate remained relatively constant over a period of 90 days at 0,22 mg/day. The serum testosterone concentration in castrated rats was 0,40 ng/ml and the value went up to 6,8 ng/ml after the biodegradable copolypeptide-testosterone composite was implanted and was kept constant for the duration of test.
    Additional Material: 8 Ill.
    Type of Medium: Electronic Resource
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  • 8
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: Biodegradable copolymers of L-lactic acid (L-LA) and DL-α-hydroxy acids with relatively low molecular weights, for example L-LA/DL-lactic acid (DL-LA), L-LA/DL-α-hydroxybutyric acid (DL-HBA), L-LA/DL-α-hydroxyisovaleric acid (DL-HIVA), and L-LA/DL-α-hydroxyisocaproic acid (DL-HICA), were synthesized by quantitative direct copolycondensation without catalysts at 200°C. The in vitro degradation, which was evaluated by measuring the weight loss of these copolymers in M/15 phosphate buffer solution (pH 7,2) without enzymes at 37°C, is strongly dependent on the kind and molecular weight of these copolymers, resulting in the formation of different degradation patterns such as parabola type (L-LA/DL-HBA system), linear type (L-LA/DL-LA system), and S type (L-LA/DL-HIVA and L-LA/DL-HICA systems).
    Additional Material: 4 Ill.
    Type of Medium: Electronic Resource
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  • 9
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: An amorphous copolyester of L-lactic acid (LA) and DL-hydroxyisocaproic acid (HICA) with a number-average molecular weight (Mn) of 1600-4800 was synthesized by direct copolycondensation in the absence of catalysts, in order to develop a biodegradable carrier for drug delivery systems. The in vivo degradation pattern was changed into an S-type from a parabolic-type with an increase in molecular weight of copolyester. A luteinizing hormone-releasing hormone agonist, des-Gly10-[D-Leu6]-LH-RH ethylamide, was incorporated into a fine cylindrical copolyester formulation by the so-called melt-pressing technique. When the S-type degradable and releasable copoly(LH/HICA) (70/30 mol-%) formulations with Mn = 2200 were implanted subcutaneously in the back of rats, the most reasonable serum drug level was observed during the first 15 weeks period, keeping constant at approximately 3,5 ng/ml.
    Additional Material: 4 Ill.
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  • 10
    Electronic Resource
    Electronic Resource
    New York : Wiley-Blackwell
    Die Makromolekulare Chemie 190 (1989), S. 1553-1559 
    ISSN: 0025-116X
    Keywords: Chemistry ; Polymer and Materials Science
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology , Physics
    Notes: The copolymerization of L-lactic acid (LA) with γ-butyrolactone (BL), performed without catalyst at 200°C under nitrogen in order to obtain a relatively low-molecular-weight copolymer, proceeds via direct condensation between linear LA and linear 4-hydroxybutyric acid produced by hydrolysis of the cyclic BL. The copolymers were characterized with respect to the copolymerizability (13C NMR spectroscopy), composition (1H NMR spectroscopy), molecular weight (terminal group analysis and gel permeation chromatography), and crystallinity (differential scanning calorimetry). The copolymerizability of BL is low, e. g., the contents of BL units in the copolymers were found to be 12, 16, and 19 mol-% for initial BL contents in the monomer feed of 30, 50, and 70 mol-%, respectively, in which copoly(LA/BL) is composed of blocks of lactyl units separated by single γ-oxybutyryl unit.
    Additional Material: 3 Ill.
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