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  • 11
    Electronic Resource
    Electronic Resource
    Effects of three histaminergic compounds on function and oxygen consumption of isolated guinea-pig hearts (1985)
    Springer
    Inflammation research 16 (1985), S. 215-218 
    Details
    ISSN: 1420-908X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract First experiences in man indicate, that even in catecholamine-insensitive congestive cardiomyopathy a considerable improvement of myocardial function can be attained by the H2-receptor agonist impromidine. In an isolated, pressure-volume work performing guinea-pig heart preparation cardiac effects of three histaminergic compounds (N α,5-dimethylhistamine (HCl)2, 5-ethyl-N α-methyl-histamine (HCl)2,N α,N α-dimethyl-histamine (HCl)2) were examined. Influences on function and myocardial oxygen consumption were compared to those obtained by impromidine. Dose-response curves for the histamine derivatives were 1.7–2.5 orders of magnitude right of the impromidine curves. Maximal inotropic stimulation was greater forN α,5-dimethyl-histamine (HCl)2 than for impromidine. All compounds exhibited a high chronotropic effect and, at high concentrations, a net coronary dilating effect.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01983143
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  • 12
    Electronic Resource
    Electronic Resource
    Histamine H3 receptor-mediated inhibition of noradrenaline release in pig retina discs (1990)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 342 (1990), S. 497-501 
    Details
    ISSN: 1432-1912
    Keywords: Pig retina ; Noradrenaline release ; Histamine H3 receptors ; R-(−)-α-Methylhistamine ; Thioperamide
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Discs of pig retina were preincubated with 3H-noradrenaline, 3H-dopamine or 3H-serotonin and then superfused. Electrical field stimulation increased the outflow of tritium from discs preincubated with 3H-noradrenaline or 3H-dopamine, but no from discs preincubated with 3H-serotonin. The tritium content at the end of superfusion was similar in discs preincubated with 3H-noradrenaline or 3H-dopamine but about tenfold lower in discs preincubated with 3H-serotonin. The tritium content in discs preincubated with 3H-noradrenaline was markedly reduced when desipramine was present during preincubation but was not affected by selective inhibitors of dopamine and serotonin uptake. The tritium content in discs preincubated with 3Hdopamine and 3H-serotonin, in contrast, was reduced or tended to be reduced by a selective dopamine and serotonin uptake inhibitor, respectively. The electrically evoked overflow of tritium from discs preincubated with 3H-noradrenaline was abolished by tetrodotoxin or omission of Ca2+. In discs superfused with desipramine, the electrically evoked overflow was enhanced by phentolamine but not affected by histamine. When both desipramine and phentolamine were present in the superfusion medium, histamine inhibited the evoked overflow (pIC15 6.85). This effect was mimicked by the histamine H3 receptor agonist R-(−)-α-methylhistamine as well as by its S-(+)-enantiomer (pIC15 7.85 and 5.30, respectively) but not by the H1 receptor agonist 2-(2-thiazolyl)ethylamine and the H2 receptor agonist dimaprit (each 10 μmol/l). The inhibitory effect of histamine was abolished by the H3 receptor antagonist thioperamide 0.32 μmol/l and attenuated by impromidine 3.2 μmol/l but not affected by the H1 receptor antagonist dimetindene 3.2 μmol/l and the H2 receptor antagonist ranitidine 10 μmol/l. The results suggest that, in the pig retina, noradrenaline is taken up into, and released from, noradrenergic neurones (most likely vascular postganglionic sympathetic nerve fibres, less probably tissue-specific noradrenergic neurones of the retina) and that noradrenaline release is subject to modulation via H3 receptors and probably also a-adrenoceptors.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00169035
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  • 13
    Electronic Resource
    Electronic Resource
    Pharmacokinetic and pharmacodynamic comparison of two doses of calcium folinate combined with continuous fluorouracil infusion in patients with advanced colorectal cancer (1999)
    Springer
    Pharmacy world & science 21 (1999), S. 184-189 
    Details
    ISSN: 1573-739X
    Keywords: Chemotherapy ; Colorectal cancer ; Fluorouracil ; Folinate ; Leucovorin ; Pharmacokinetics ; Toxicity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The optimum dose of calcium folinate (leucovorin) as modulator of fluorouracil has not been defined yet. We conducted a randomized trial to compare the pharmacokinetics/pharmacodynamics of two doses of calcium folinate. 16 patients with advanced colorectal cancer were treated with 650 mg/m2/d fluorouracil as 5 day continuous infusion and randomized to receive either 20 mg/m2 or 100 mg/m2 calcium folinate as short infusion twice daily. The two diastereoisomers of calcium folinate were analyzed separately by chiral HPLC to account for differences in their pharmacokinetics. The pharmacokinetics of fluorouracil was not affected by folinate dosing. Total clearance of the active (6S)-diastereoisomer was found to be lower after the higher dose of folinate which can be explained by nonlinear metabolism. The incidence of treatment‐induced mucositis significantly increased with (6S)‐folinate exposure, whereas fluorouracil exposure was not related to this type of toxicity. In conclusion, exposure to folinate is more important for toxicity in this regimen than fluorouracil pharmacokinetics. Therefore, monitoring of fluorouracil plasma levels is not useful in this combination. Our results show that folinate dose should be carefully selected. Lower doses of folinate might be preferred because of less toxicity compared to higher doses.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1008671129128
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  • 14
    Electronic Resource
    Electronic Resource
    Development and Application of a Simple Assay to Quantify Cellular Adducts of Platinum Complexes with DNA (1999)
    Springer
    Pharmaceutical research 16 (1999), S. 470-473 
    Details
    ISSN: 1573-904X
    Keywords: platinum-DNA adducts ; platinum complexes ; cisplatin ; carboplatin ; pharmacodynamics ; anticancer drugs
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1011950524701
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  • 15
    Electronic Resource
    Electronic Resource
    7,8-Dihydroimidazo[1,2-c]pyrimidin-5(6H)-one, -5(6H)-thione und -5(6H)-ylidencyanamide (1984)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 117 (1984), S. 2597-2614 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: 7,8-Dihydroimidazo[1,2-c]pyrimidine-5(6H)-ones, -5(6H)-thiones, and -5(6H)-ylidenecyanamidesThe cyclisation of the 4,5-substituted 2-(2-aminoethyl)imidazoles 5 with dimethyl N-cyanodithioimidocarbonate (2), 1,1′-carbonyldiimidazole (10a), or 1,1′-thiocarbonyldiimidazole (10b) gives the hitherto unknown title compounds 7, 11, and 14. The 1H and 13C NMR data as well as the reactions with nucleophiles are described.
    Notes: Die Cyclisierung der 4,5-substituierten 2-(2-Aminoethyl)imidazole 5 mit Dimethyl-N-cyandithioimidocarbonat (2), 1,1′-Carbonyldiimidazol (10a) oder 1,1′-Thiocarbonyldiimidazol (10b) ergibt die bisher nicht beschriebenen Titel-Verbindungen 7, 11 und 14. Die 1H- und 13C-NMR-Daten sowie des Verhalten gegenüber Nucleophilen werden beschrieben.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19841170805
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  • 16
    Electronic Resource
    Electronic Resource
    Nicethamid-Analoge, VII. Darstellung eines nicethamid-analogen Pyrrolo [3,4-b]- und Pyrrolo [3,4-c]pyridinons (1975)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 108 (1975), S. 1003-1009 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Nicethamide-Analogues, VII. Synthesis of a Pyrrolo[3,4-b]- and Pyrrolo [3,4-c]pyridinone as Nicethamide AnaloguesThe synthesis of the potentially analeptically active cyclic nicethamide analogues, 6-ethyl-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-one(9a) and 2-ethyl-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-3-one (9b) as well as the corresponding open-ring compounds N-ethyl-2-methylnicotinamide (12a) and N-ethyl-4-methylnicotinamide (12b) is described.
    Notes: Die Synthese der potentiell analeptisch wirksamen cyclischen Nicethamid-Analoga 6-Äthyl-6,7-dihydro-5H-pyrrolo[3,4-b]pyridin-5-on (9a) und 2-Äthyl-2,3-dihydro-1H-pyrrolo[3,4-c]pyridin-3-on (9b) sowie der entsprechenden ringoffenen Verbindungen N-Äthyl-2-methylnicotinamid (12a) and N-Äthyl-4-methylnicotinamid (12b) wird beschrieben.
    Additional Material: 2 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19751080404
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  • 17
    Electronic Resource
    Electronic Resource
    Nicethamid-Analoge, V Untersuchungen zur gehinderten internen Rotation bei N,N-Dimethylpyridinamiden (1975)
    Weinheim : Wiley-Blackwell
    Berichte der deutschen chemischen Gesellschaft 108 (1975), S. 730-734 
    Details
    ISSN: 0009-2940
    Keywords: Chemistry ; Inorganic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Nicethamide Analogues, V. Investigations of Hindered Internal Rotation in N,N-DimethylpyridinamidesThe synthesis of homologue, vinylogue and ringalkylated N,N-dimethyl nicotinamides is described and the energy barrier of the hindered rotation of the amide group determined by means of 1H-n. m. r. spectroscopy.
    Notes: Die Synthese von homologen, vinylogen und Kernalkylierten N,N-Dimethylnicotinamiden wird beschrieben und die Energiebarriere bei der gehinderten Rotation der Amidgruppe mittels 1H-NMR-Spektroskopie bestimmt.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/cber.19751080303
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  • 18
    Electronic Resource
    Electronic Resource
    Zur Synthese von (Z)- und (E)-3-(1H-Imidazol-4-yl)-2-propenamin und einigen 3-(1H-Imidazol-4-yl)propanaminen (1992)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1992 (1992), S. 317-323 
    Details
    ISSN: 0170-2041
    Keywords: Homohistamine ; Imidazole derivatives ; 2-Propenamine derivatives ; Impromidine ; Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Notes: Synthesis of (Z)- and (E)-3-(1H-imidazol-4-yl)-2-propenamine and Some 3-(1H-imidazol-4-yl)propanamines3-(1H-Imidazol-4-yl)propanamine (6, homohistamine), an essential intermediate for the synthesis of potent impromidine-type histamine H2 receptor agonists, is efficiently prepared from trans-urocanic acid (1) by reduction of the methyl ester 2 and conversion to the saturated amide 4. Dehydration with thionyl chloride yields the nitrile 5 which is subsequently reduced to 6. Side-chain methylated 3-(1H-imidazol-4-yl)propanamines 12 are available from 1H-imidazole-4-carbaldehyde (7) and 1-(1H-imidazol-4-yl)ethanone (8), respectively, via unsaturated nitriles 10 and stepwise reduction. Cyclization of the appropriate 4-bromo-5-oxohexanenitriles 14α with formamidine in liquid ammonia and reduction of the obtained nitriles 15 furnishes ring-methylated amines 16. (E)-3-(1H-Imidazol-4-yl)-2-propenamine [(E)-23] is obtained in six steps from the trans-ester 2 while (Z)-23 is accessible by treating 7 with triphenyl(2-phthalimidoethyl)phosphonium bromide (17) and final deprotection. These primary amines are valuable intermediates for the synthesis of impromidine analogues.
    Additional Material: 1 Tab.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.199219920158
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  • 19
    Electronic Resource
    Electronic Resource
    Racemattrennung, Kristallstruktur und histaminartige Wirkung von 4-[1-(2-Aminoethylthio)ethyl]-5-methylimidazol (1983)
    Weinheim : Wiley-Blackwell
    Liebigs Annalen 1983 (1983), S. 678-683 
    Details
    ISSN: 0170-2041
    Keywords: Chemistry ; Organic Chemistry
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Resolution, Crystal Structure, and Histamine-like Activity of 4-[1-(2-Aminoethylthio)ethyl]-5-methylimidazoleThe resolution of racemic 4-[1-(2-aminoethylthio)ethyl]-5-methylimidazole (1) using optically active Di-O-(P-toluoyl)tartaric acid as well as the histamine-like activity of the enantiomers are described. The crystal structure of (+)-1 · 2HCl · H2O has been determined and refined until R = 0.0483. Accordingly, (+)-1 is R configurated. Only (S)-(-)-1 possesses H1-agonistic activity.
    Notes: Es wird die Racemattrennung von 4-[1-(2-Aminoethylthio)ethyl]-5-methylimidazol (1) mittels optisch aktiver Di-O-(p-toluoyl)weinsäure sowie die histaminartige Wirksamkeit der Enantiomeren beschrieben. Von (+)-1 · 2HCl · H2O wurde die Kristallstruktur bestimmt und bis zu einem R-Wert von 0.0483 verfeinert. Danach ist (+)-1 R-konfiguriert. Von den beiden Enantiomeren besitzt nur (S)-(-)-1 H1-agonistische Aktivität.
    Additional Material: 1 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/jlac.198319830416
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  • 20
    Electronic Resource
    Electronic Resource
    Quantitative trace analysis of interleukin-3, interleukin-6, and basic model proteins using isotachophoresis-capillary zone electrophoresis with hydrodynamic counterflow (1998)
    Weinheim : Wiley-Blackwell
    Electrophoresis 19 (1998), S. 305-310 
    Details
    ISSN: 0173-0835
    Keywords: Capillary electrophoresis ; Isotachophoresis ; Proteins ; Interleukins ; Chemistry ; Biochemistry and Biotechnology
    Source: Wiley InterScience Backfile Collection 1832-2000
    Topics: Biology , Chemistry and Pharmacology
    Notes: A quantitative analytical technique to determine trace concentrations of recombinant human interleukin-3 (rhIL-3), recombinant human IL-6 (rhIL-6), and various basic model proteins is described using isotachophoresis-capillary zone electrophoresis (ITP-CZE). Proteins were separated on coated fusedsilica capillaries using a commercial capillary electrophoretic system modified for the application of isotachophoretic preconcentration with hydrodynamic counterflow. The effect of injection time and isotachophoretic focusing time was investigated and compared with predictions from existing mathematical models. Good linearity of the calibration graphs (r 〉 0.995) was observed for all investigated proteins. The limit of quantification was in the 10-8 M range using UV detection at 200 nm. Within-day and between-day precison of peak area ranged between 1 and 6%. Precision was unaffected by isotachophoretic preconcentration. In conclusion, the described method is feasible to quantify trace concentrations of rhIL-3, rhIL-6, and basic proteins. Potential applications comprise issues of pharmaceutical quality control.
    Additional Material: 5 Ill.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1002/elps.1150190227
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