Library

feed icon rss

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
  • 1
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 239 (1960), S. 475-480 
    ISSN: 1432-1912
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Schlußfolgerungen und Zusammenfassung Die Befunde stimmen mit denjenigen von Corda überein. Sie stehen im Gegensatz zu den Befunden von Freerksen, welcher eine Spezifität einiger Organe bei der Spaltung des Antibioticums beobachtet hatte. Dieser Unterschied kann zum Teil seine Erklärung in den verschiedenen Konzentrationen des verwendeten Cycloserins (500 bis 1000 γ/cm3 bei den Untersuchungen von Freerksen und 60 γ/cm3 bei den unsrigen) und in der Verschiedenheit der Tierarten, welche verwendet wurden, finden. So hat z.B. Freerksen nachgewiesen, daß die Resorption nach peroraler Verabfolgung bei der Maus äußerstschnell und beim Kaninchen sehr langsam vor sich geht. Die von Freerksen verwendeten hohen Dosen könnten jedoch eine geringfügige Spaltung verschleiern. Die fehlende Spaltung des Antibioticums in durch Hitze enteiweißten Leber-Homogenaten erlaubt die Schlußfolgerung, daß die Spaltung von enzymatischem Charakter ist. Die Derivate des Cycloserins, welche nach der Methode von Jones eine Färbung geben, haben einen intakten basischen Ring: z.B. Monoacetyl-und Desamino-Cycloserin (Jones). Es ist deshalb anzunehmen, daß der fehlenden Reaktion mit Nitroprussid, auf Grund derer wir glauben, daß es zum Abbau gekommen ist, eine Öffnung des Oxazol-Ringes entspricht. Andererseits schließt Conzelmann beim Affen die Bildung des Acetyl-Derivates aus. Nach Freerksen soll es zur Öffnung des Ringes (vielleicht durch eine Cycloamidase) unter Bildung von Serin, Stickstoff, Wasser und Ammoniak kommen. 1. Cycloserin bei einmaligern Verabfolgung zeigt keine besondere Affinität zu den untersuchten Organen. 2. Bei der Ratte wird die gute Resorption von Seiten des Magen-Darm-Traktes bestätigt; die Verteilung des Pharmakons in den Geweben scheint unabhängig von der Art der Verabreichung zu sein. 3. Auch bei wiederholter Behandlung scheint weder eine besondere Organaffinität, noch eine Kumulation aufzutreten. 4. In der Leber findet sich das Antibioticum vorwiegend in der Supernatantschicht der zentrifugierten Homogenate. 5. Unter den verschiedenen Leber-Fraktionen sollen die Mitochondrien die größte Stoffwechsel-Aktivität haben. Es ist nicht möglich, zu entscheiden, ob die geringe Konzentration in den Mitochondrien einer geringen Eindringung des Antibioticums in diese oder einer intensiven Spaltung zuzuschreiben ist. 6. Cycloserin wird außer von der Leber auch von zahlreichen anderen Geweben gespalten: Lunge, Nirer, Gehirn und Muskel.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    Electronic Resource
    Electronic Resource
    Springer
    European journal of clinical pharmacology 25 (1983), S. 135-137 
    ISSN: 1432-1041
    Keywords: phenytoin ; drug interactions ; cimetidine ; inhibition of metabolism ; disposition kinetics ; mixed function oxidases
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The effect of cimetidine on the disposition kinetics of phenytoin was investigated in 7 healthy volunteers. Each subject received a single intravenous dose of phenytoin on two occasions, in the control state, and during concurrent treatment with cimetidine 1200 mg/day for 6 days. A slight but statistically significant decrease both in the rate of elimination and total body clearance of phenytoin was observed during the administration of cimetidine. The effect is probably due to inhibition of metabolism.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    ISSN: 1432-1912
    Keywords: Peristaltic reflex ; Intestinal motility ; Sympathetic denervation ; Supersensitivity ; Adrenoceptors
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 1. The concentration-effect relationships of adrenergic agonists in inhibiting muscular tone, carbachol-induced contraction of circular muscle strips and nerve-mediated motor activity during the peristaltic reflex have been studied in intact and sympathetically denervated preparations of isolated guinea-pig colon. 2. The order of potencies of adrenergic agonists was different for muscular and nerve-mediated effects, being clonidine 〉 noradrenaline 〉 methoxamine 〉 isoprenaline for the inhibition of peristalsis and isoprenaline 〉 noradrenaline 〉 methoxamine 〉 clonidine for the relaxation of circular muscle. 3. Denervation supersensitivity was specific for the adrenergic agonists and developed both to the muscular and nerve-mediated effects, involving both α and β receptors. The degree of potentiation was similar for noradrenaline and isoprenaline when measured for the muscular effects but was significantly higher for noradrenaline than for isoprenaline or methoxamine when measured for peristalsis inhibition. No potentiation could be observed for papaverine and for the muscular effects of methoxamine and phenylephrine. The increase in potency of noradrenaline ranged from a 26-fold increase for the inhibition of propulsion velocity to a 2.5-fold increase for the inhibition of carbachol-induced contraction. A much narrower range was observed for isoprenaline. Potentiation could also be observed for the inhibitory effect of noradrenaline on acetylcholine release. 4. Clonidine was the most potent agonist against peristaltic reflex and the weakest agonist in relaxing circular muscle. Denervated preparations became subsensitive to the inhibitory effect of clonidine on peristaltic reflex. The potency of clonidine relative to noradrenaline was 488 in intact preparations and only 3.1 in denervated organs. 5. Our results are consistent with a main role played by β receptors in the relaxation of circular smooth muscle and with a selective involvement of α2 receptors in peristalsis inhibition. The pattern of sensitivity changes is consistent with a high degree of physiological modulation by sympathetic supply both on the smooth muscle and on the intramural nervous structures. Both pre- and postjunctional mechanisms could be responsible for the development of supersensitivity, but the former seem to operate only at interneuronal synapses. The opposite sensitivity changes observed for noradrenaline and clonidine suggest a different effect of two agonists at the presynaptic level.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 4
    Electronic Resource
    Electronic Resource
    Springer
    Naunyn-Schmiedeberg's archives of pharmacology 324 (1983), S. 180-184 
    ISSN: 1432-1912
    Keywords: GABA ; 5-Hydroxytryptamine ; Guinea-pig ileum ; Desensitization
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary 1. GABA (3–100 μM) and 5-HT (0.03–30 μM) caused concentration-dependent transient contractions of the longitudinal muscle of the guinea-pig ileum. 2. The contractile response to GABA was antagonized by hyoscine (2.2 μM), TTX (0.7 μM), bicuculline (3 μM), furosemide (25 μM) and desensitization to GABA itself, while hexamethonium (20 μM) and methysergide (20 μM) were without effect. 3. The contractile response to 5-HT was antagonized by hyoscine (2.2 μM), TTX (0.7 μM) and desensitization to 5-HT itself and was unaffected by bicuculline (10 μM), hexamethonium (20 μM), furosemide (25 μM) and methysergide (20 μM). 4. A desensitization procedure that caused a 84.7-fold increase in the 5-HT EC50 also resulted in a 74.1-fold increase of the GABA EC50. Desensitization to GABA caused a reduction of 5-HT induced response but only in preparations desensitized by high (50 μM) concentrations of GABA. 5. The results indicate that GABA-induced contractions in the guinea-pig ileum are mediated by activation of cholinergic motor neurones. This effect appears to be mediated by interneuronal release of 5-HT rather than by a direct stimulatory action of GABA on the effector neurones.
    Type of Medium: Electronic Resource
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...