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  • 1
    Electronic Resource
    Electronic Resource
    QSAR and conformational analysis of the antiinflammatory agent amfenac and analogues (1993)
    Springer
    Journal of computer aided molecular design 7 (1993), S. 183-198 
    Details
    ISSN: 1573-4951
    Keywords: QSAR ; Conformational analysis ; Prostaglandin synthase ; Antiinflammatory ; Amfenac
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Summary The new nonsteroidal antiinflammatory drug (NSAID) arylacetic amfenac (2-amino-3-benzoylphenylacetic acid) and 19 substituted derivatives were studied in order to correlate the biological activities with the structure-related parameters. The geometry of amfenac in neutral and anionic form was totally optimized, starting from standard geometries and crystallographic data, using semiempirical AM1 and MNDO quantum-mechanical methods. Conformational analysis shows the existence of a rigid structure for rotations of the acetic acid chain (α°) and the central carbonyl group (γ°) around the bonds with the phenylamine ring, whereas the carboxyl group (β°) and the phenyl ring of the benzoyl group (δ°) can rotate almost freely. Electrostatic potential maps were analyzed and showed that the electrostatic orientation effect seems to make an important contribution to the binding of the active compounds to prostaglandin synthase. An electrostatic orientation model of the binding site is proposed. The frontier orbital charge distribution was also described for each compound. On the other hand, steric, electronic and hydrophobic (log P) parameters were calculated and QSAR analysis showed that the most significant parameter for the antiinflammatory activity was the π-electron density of the HOMO orbital in the second aromatic ring. These results suggest a possible electronic charge transfer between the aromatic fragments and the receptor.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00126444
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    Paper (German National Licenses)
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  • 2
    Electronic Resource
    Electronic Resource
    Antiarrhythmic actions of clemizole as pharmacologic evidence for a circus movement mechanism in atrial flutter (1969)
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 262 (1969), S. 325-336 
    Details
    ISSN: 1432-1912
    Keywords: Clemizole ; Arrhythmia ; Antihistaminics ; Cell Membrane
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary The antihistaminic clemizole was studied as an antiarrhythmic in a preparation in which two arrhythmias of different nature and mechanism were produced in the right atrium of anesthetized dogs. One of the arrhythmias was a circus movement flutter induced by the method of Rosenblueth and García Ramos; the other, an ectopic focus induced by local application of aconitine in the auricular appendage, electrically isolated from the rest of the atrium. Clemizole selectively converted the flutter to sinus rhythm with little action on the coexistent aconitine dysrhythmia. It did not modify arterial pressure. In effective doses the wave length of the impulse was increased by prolongation of the refractory period without significant reduction in conduction velocity. Similarly, in subendocardial cells of isolated rat atria, clemizole in appropriate concentrations retards repolarization with little effect on the rate of depolarization. These results afford pharmacological evidence for the existence of atrial circus movement arrhythmias which can respond to prolongation of the refractory period unaccompanied by effects on other properties of the tissue. Other arrhythmias, self-sustained by the discharge of an ectopic focus, such as the tachysystole produced by aconitine, are not suppressed by similar increase in the refractory period.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00538434
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    Paper (German National Licenses)
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  • 3
    Electronic Resource
    Electronic Resource
    Soybean aeroallergen around the port of New Orleans: A potential cause of asthma (1996)
    Springer
    Aerobiologia 12 (1996), S. 173-176 
    Details
    ISSN: 1573-3025
    Keywords: Aeroallergen ; Soybean asthma ; Immunochemical Assay ; Air sampling
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract There have been reported epidemics of severe asthma in Barcelona, Spain, linked to a 10 kDa low molecular mass (LMM) allergen from soybean hulls that became airborne during unloading of ships. As a preliminary probe of the potential for dispersion of this allergen in USA cities, four automated air samplers were placed around a grain elevator in New Orleans and operated continuously from May to October 1990. The allergen was extracted from the filters and immunochemically assayed for soybean aeroallergen. On 31 separate days, the airborne allergen concentration in at least one of the samples was over 10000 U/m3 similar to those observed in Barcelona on some epidemic days. Areas North and East of the elevator were most affected. Serologie studies showed that of 50 asthmatics from New Orleans who were participants in an unrelated clinical study 4 or 8% demonstrated elevated titers of IgE antibody to LMM soybean allergen. Only 1 of 475 control sera (half of which were also asthmatic) obtained elsewhere in the US was positive for LMM soybean IgE antibody. Based on the findings in this study, there is a great possibility that on some days there is enough soybean allergen in the air and a sufficient frequency of soybean aeroallergen RAST positive asthmatics in New Orleans to warrant further investigation of the contribution of soybean aeroallergen to asthma around the port of New Orleans.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02248146
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
    Fulltext
  • 4
    Electronic Resource
    Electronic Resource
    Soybean aeroallergen around the port of New Orleans: a potential cause of asthma (1996)
    Springer
    Aerobiologia 12 (1996), S. 173-176 
    Details
    ISSN: 1573-3025
    Keywords: Aeroallergen ; Soybean asthma ; Immunochemical Assay ; Air sampling
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract There have been reported epidemics of severe asthma in Barcelona, Spain, linked to a 10 kDa low molecular mass (LMM) allergen from soybean hulls that became airborne during unloading of ships. As a preliminary probe of the potential for dispersion of this allergen in USA cities, four automated air samplers were placed around a grain elevator in New Orleans and operated continuously from May to October 1990. The allergen was extracted from the filters and immunochemically assayed for soybean aeroallergen. On 31 separate days, the airborne allergen concentration in at least one of the samples was over 10 000 U/m3, similar to those observed in Barcelona on some epidemic days. Areas North and East of the elevator were most affected. Serologic studies showed that of 50 asthmatics from New Orleans who were participants in an unrelated clinical study 4 or 8% demonstrated elevated titers of IgE antibody to LMM soybean allergen. Only 1 of 475 control sera (half of which were also asthmatic) obtained elsewhere in the US was positive for LMM soybean IgE antibody. Based on the findings in this study, there is a great possibility that on some days there is enough soybean allergen in the air and a sufficient frequency of soybean aeroallergen RAST positive asthmatics in New Orleans to warrant further investigation of the contribution of soybean aeroallergen to asthma around the port of New Orleans.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF02447409
    Library Location Call Number Volume/Issue/Year Availability
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    Paper (German National Licenses)
    Fulltext
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