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  • Articles: DFG German National Licenses  (8)
  • Chemistry  (6)
  • Colorectal cancer  (1)
  • Folinate  (1)
  • Guinea-pig and mouse brain slices  (1)
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  • Articles: DFG German National Licenses  (8)
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  • 1
    Electronic Resource
    Electronic Resource
    H2 receptor-mediated facilitation and H3 receptor-mediated inhibition of noradrenaline release in the guinea-pig brain (1998)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 357 (1998), S. 232-239 
    Details
    ISSN: 1432-1912
    Keywords: Key words H2 and H3 receptors ; Noradrenaline release ; Guinea-pig and mouse brain slices ; Presynaptic ; receptors ; Impromidine ; Sopromidine ; Ranitidine ; Clobenpropit
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effect of histamine and related drugs on the tritium overflow evoked electrically (0.3 Hz) or by introduction of Ca2+ ions into Ca2+-free K+-rich (25 mmol/l) medium containing tetrodotoxin was studied in superfused guinea-pig brain cortex, cerebellum, hippocampus or hypothalamus slices and in mouse brain cortex slices preincubated with 3H-noradrenaline. The electrically evoked tritium overflow in guinea-pig cortex slices was inhibited by histamine; the H3 receptor antagonist clobenpropit reversed the effect of histamine to a slight facilitation. The facilitatory effect of histamine (obtained in the presence of clobenpropit) was not affected by the H1 receptor antagonist mepyramine but abolished by the H2 receptor antagonist ranitidine. In the absence of clobenpropit, ranitidine augmented the inhibitory effect of histamine. In slices superfused in the presence of ranitidine, the evoked overflow was inhibited by histamine and, more potently, by the H3 receptor agonist R-α-methylhistamine in a concentration-dependent manner (maximum inhibitory effect obtained for both agonists 30–35%). The concentration-response curve of histamine was shifted to the right by the H3 receptor antagonist thioperamide. R-α-Methylhistamine inhibited the electrically evoked tritium overflow also in guinea-pig cerebellar, hippocampal and hypothalamic slices. In cortex slices superfused in the presence of clobenpropit, the H2 receptor agonists impromidine and, less potently, R-sopromidine facilitated the evoked overflow in a concentration-dependent manner. S-Sopromidine only tended to increase the evoked overflow. The effect of impromidine was counteracted by the H2 receptor antagonists ranitidine and cimetidine. The extent of the maximum facilitatory effect of impromidine (by 15–20%) was about the same when (i) the Ca2+ concentration in the medium was reduced from 1.3 to 0.98 mmol/l, (ii) the time of exposure to impromidine was reduced from 28 to 8 min or (iii) cerebellar, hippocampal or hypothalamic slices were used instead of cortical slices. The Ca2+-induced tritium overflow in guinea-pig cortex slices was inhibited by histamine (in the presence of ranitidine); this effect was abolished by clobenpropit. In slices superfused in the presence of clobenpropit, impromidine failed to facilitate the Ca2+-evoked tritium overflow. The electrically evoked tritium overflow in mouse brain cortex slices was inhibited by histamine by about 60% (both in the absence or presence of ranitidine). The inhibitory effect of histamine was abolished (but not reversed) by clobenpropit. In conclusion, noradrenaline release in the guinea-pig brain cortex is inhibited via presynaptic H3 receptors and facilitated via H2 receptors not located presynaptically. In the mouse brain cortex, only inhibitory H3 receptors occur. The extent of the H3 receptor-mediated effect is more marked in the mouse than in the guinea-pig brain cortex.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/PL00005162
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    Paper (German National Licenses)
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  • 2
    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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    Paper (German National Licenses)
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  • 3
    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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    Paper (German National Licenses)
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  • 4
    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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  • 5
    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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  • 6
    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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  • 7
    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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  • 8
    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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