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  • 1
    Electronic Resource
    Electronic Resource
    s.l. : American Chemical Society
    Journal of the American Chemical Society 103 (1981), S. 4992-4996 
    ISSN: 1520-5126
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 2
    Electronic Resource
    Electronic Resource
    s.l. : American Chemical Society
    Journal of the American Chemical Society 102 (1980), S. 4889-4893 
    ISSN: 1520-5126
    Source: ACS Legacy Archives
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 3
    Electronic Resource
    Electronic Resource
    Springer
    Inflammation research 44 (1995), S. 548-555 
    ISSN: 1420-908X
    Keywords: Meloxicam ; Piroxicam ; Diclofenac ; Adjuvant arthritis ; Lewis rat
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The effects of meloxicam, piroxicam, diclofenac and tenidap on the swelling of hind paws, radiologically-detectable bone and cartilage destruction of hind paws, increase in spleen weight, increase in erythrocyte sedimentation rate and changes in serum protein composition in male Lewis rats with adjuvant arthritis were studied following once-daily oral administration of these drugs for 21 days. All the drugs dose-dependently inhibited hind paw swelling. For equal activity against hind paw swelling caused by the secondary reaction, the required daily dose of piroxicam was about twice that of meloxicam; those of diclofenac and tenidap were about 3.5 and 60 times higher respectively. The bone and cartilage destruction induced by adjuvant arthritis were inhibited by meloxicam at low daily doses and by piroxicam at doses approximately four times those of meloxicam. Diclofenac and tenidap had only a weak effect on radiologically-detectable lesions when administered at doses sufficient to reduce paw swelling. Meloxicam also had a dose-dependent corrective effect on the systemic changes which occur in adjuvant arthritic rats, e.g. increase in spleen weight, increase in erythrocyte sedimentation rate and changes in serum protein composition. Piroxicam produced similar effects, at 3–4 times higher doses. Diclofenac and tenidap did not show comparable effects when administered at appropriate doses. These findings indicate that the action of meloxicam and piroxicam differs from that of diclofenac and tenidap in adjuvant arthritis in the Lewis rat. At oral doses which significantly reduce edema formation, only meloxicam and piroxicam showed a significant effect on systemic parameters of adjuvant disease in the Lewis rat.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1420-908X
    Keywords: Meloxicam ; Non-steroid anti-inflammatory drugs ; Anti-inflammatory activity ; Analgesic activity ; Gastrointestinal tolerance
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract The anti-inflammatory, analgesic and antipyretic properties of the new non-steroidal anti-inflammatory agent, meloxicam, were investigated in a variety of animal models and compared with the properties of piroxicam, diclofenac, indomethacin and several other NSAIDs. With respect to the total effect of a single oral dose, the anti-exudative effect of meloxicam on carrageenaninduced oedema in the rat exceeded that of all the NSAIDs included in the comparison. Additionally, meloxicam showed the greatest potency of all the compounds examined with respect to adjuvant-induced arthritis in the rat, the granuloma pouch model and the cotton pellet test in the rat. Unlike indomethacin, in the carrageenan pleurisy model in the rat, meloxicam caused both a dose-dependent reduction in exudate volume and also inhibition of leucocyte migration. Meloxicam showed a strong and lasting effect on inflammatory pain in the rat. Like other NSAIDs, but unlike dipyrone, meloxicam had no effect in the hot plate and tail clamp tests, which are used to identify weak central analgesic effects. Unlike dipyrone and like indomethacin, meloxicam had no effect in a model of visceral distention pain. In common with other NSAIDs, meloxicam had no influence on the body temperature of normothermic rats in the anti-inflammatory dose range, but did reduce yeastinduced fever in the rat in a dose-dependent manner. Like piroxicam, meloxicam had a uricosuric effect on rats treated with oxonic acid. Low-dose meloxicam inhibited both bradykinin-induced and PAF-induced bronchospasm in the guinea-pig, but had no effect on acetylcholine-induced bronchospasm. Piroxicam had greater ulcerogenic effects in the rat stomach than meloxicam. The therapeutic range of meloxicam in the rat, with regard to inhibition of adjuvant arthritis, was several times greater than that of piroxicam, indomethacin, diclofenac and naproxen.
    Type of Medium: Electronic Resource
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  • 5
    ISSN: 1420-908X
    Keywords: Key words: Cyclooxygenase — COX-1 — COX-2 — Non-steroidal anti-inflammatory drugs (NSAIDs)
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Abstract. Objective and Design: Two structurally related compounds, meloxicam (Mel) and its structural 4′-isomer (4′-Mel), were compared to examine the role of a slightly different chemical structure on cyclooxygenase (COX) selectivity in in vitro and in vivo experimental models.¶Material or Subjects: In vitro studies were performed using human whole blood obtained from healthy volunteers, in vivo studies were performed in rats.¶Treatment: A concentration-response curve was obtained in the whole blood assay for Mel, 4′-Mel, indomethacin, piroxicam and diclofenac. These were used to calculate the respective IC50 values of either prostaglandin E2 (PGE2) or thromboxane B2 (TxB2). Similarly, a dose-response curve was obtained for Mel, 4′-Mel and piroxicam when measuring in vivo prostaglandin production, anti-inflammatory activity and gastric tolerance to determine the dose resulting in a 50% reduction of the each parameter.¶Methods: COX selectivity was investigated in vitro using a human whole blood assay. PGE2 synthesis in vivo was measured in inflammatory exudate, in the stomach and kidneys of rats. Anti-inflammatory effects were measured in an adjuvant arthritis model and gastric tolerance was tested in an ulcerogenicity model in vivo in rats.¶Results: In the human whole blood assay, the ratio of IC50 values for COX-1 vs. COX-2 inhibition was 13 for Mel and 1.8 for 4′-Mel. In inflammatory exudate in rats, Mel and 4′-Mel inhibited PGE2 synthesis to a similar extent, ID50 values ∼ 0.3 mg/kg. In contrast, Mel was a weaker inhibitor of PG synthesis than 4′-Mel in the rat stomach and in the rat kidney. Paw swelling was reduced by 50% with 0.1 and 0.2 mg/kg for Mel and 4′-Mel, respectively, in the rat adjuvant arthritis model. Gastric tolerance (UD50) was 2.4 mg/kg for Mel and 0.4 mg/kg for 4′-Mel.¶Conclusions: These data demonstrate that the in vitro and in vivo pharmacological profile of meloxicam is structurally dependent and that minor structural changes can lead to significant differences in the selectivity for COX-1 and COX-2 in vitro and to different profiles in vivo suggesting different therapeutic potential.
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Springer
    Medical microbiology and immunology 41 (1902), S. 244-256 
    ISSN: 1432-1831
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Springer
    Archives of microbiology 93 (1973), S. 229-237 
    ISSN: 1432-072X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary Among various soil microorganisms tested only Pseudomonas putida isolate 1065 and Rhizopus japonicus ATCC 24794 were able to transform o-toluate. In P. putida o-toluate was quantitatively hydroxylated to give 2-hydroxymethyl-benzoate and in R. japonicus it was reduced to 2-hydroxymethyltoluene. Both compounds, which were identified on the basis of their physical properties, accumulated during a one week growth period.
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Springer
    Archives of microbiology 114 (1977), S. 25-33 
    ISSN: 1432-072X
    Keywords: Substituted phenols ; Insecticides ; “Meta”fission ; Nocardia
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract 4-(Methylmercapto)-phenol (MMP) and 4-(methylsulfinyl)-phenol (MSP) are oxidized by the soil isolate Nocardia spec. DSM 43251, which is closely related to Nocardia calcarea. The rate of degradation depends on the capability of a substrate to support growth and is strongly enhanced in the presence of a second carbon source under the conditions of cooxidation. MMP and MSP are cometabolized by hydroxylation of the benzene ring with the formation of the substituted catechol following by ring cleavage between carbon atoms 2 and 3 (“meta”fission) to give 2-hydroxy-5-methylmercapto-or 2-hydroxy-5-methylsulfinylmuconic semialdehyde. Oxidation of MMP to MSP represents a bypath of MMP-oxidation. The intermediates were identified on the basis of their physical properties. The enzymes responsible for the metabolism of MMP and MSP are induced by growth with MMP or MSP, but not with glucose. MMP- and MSP-induced cells catalyze the oxidation of a variety of substituted phenols. This indicates a rather low substrate specificity of the enzymes induced by MMP and MSP.
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Springer
    Archives of microbiology 80 (1971), S. 315-323 
    ISSN: 1432-072X
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Description / Table of Contents: Zusammenfassung Die Acylanilide Monalide, Carboxin, Oxycarboxin, 2,5-Dimethylfurancarbonsäureanilid, Pyracarbolid, 2-Methyl- und 2-Chlorbenzoesäureanilid, der N′-Phenylcarbaminsäureester Propham und die N-Phenylharnstoff-derivate Monolinuron, Linuron, Metobromuron und Maloran wurden durch B. sphaericus an der Amidbindung zu den entsprechenden Anilinen und Säuren gespalten. Der qualitative Nachweis der Zwischenprodukte gelang dünnschicht- und gaschromatographisch mit Hilfe von Vergleichssubstanzen. Für den Abbau der Phenylamide durch B. sphaericus wurde ein Abbauschema aufgestellt.
    Notes: Summary B. sphaericus is degrading the acylamides monalide, carboxin, oxycarboxin, 2,5-dimethylfurancarboxylic acid anilide, pyracarbolid, 2-methyl-and 2-chloro-benzoic acid anilide, the N′-phenylcarbamate propham and the N′-methoxyphenylurea compounds monolinuron, linuron, metabromuron and maloran by cleaving the amide linkage, forming the corresponding anilines and acids. The metabolites were determined qualitatively by the means of co-thinlayer- and co-gaschromatography. A pathway for degradation of the phenylamides by B. sphaericus is proposed.
    Type of Medium: Electronic Resource
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  • 10
    ISSN: 1432-072X
    Keywords: Arylamine N-acetyltransferase ; Metabolism of aromatic amines ; Soil microorganisms ; Bacillus cereus
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The raw extracts of a series of microorganisms were screened for the presence of acetyl-coenzyme A: arylamine N-acetyltransferase (AAAT) using a radioactive assay with 3H-acetyl-coenzyme A and aniline as substrates. Enzyme activities were primarily detected in the soluble fractions of Bacillus and Nocardia species, and in some further soil organisms. Only strains of Bacillus cereus were able to acetylate 4-nitroaniline and 3,5-dimethyl-4-nitroaniline. The fermentation conditions for the production of the enzyme were optimized. The AAAT from one strain of Bacillus cereus was purified 24-fold and characterized.
    Type of Medium: Electronic Resource
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