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  • 1
    ISSN: 1432-0428
    Keywords: Insulin secretionin vivo andin vitro ; hypoglycaemic sulphonamide ; oral antidiabetic substances ; RP 22410 ; tolbutamide ; insulin secretion stimulator ; islets of Langerhans ; islet development ; beta cells ; betacytotrophic action ; Glisoxepid
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Résumé Le glisoxepid ou RP 22410 est un nouveau sulfonylurée hypoglycémiant très actif. Chez le chien normal éveillé, administré par voie intraveineuse, il est 81 ou 131 fois plus actif que le tolbutamide, suivant que les doses sont exprimées en poids ou en moles. Cette action hypoglycémiante ne se manifeste pas chez le chien totalement dépancréaté. — Ce produit stimule la sécrétion d'insuline.In vivo chez le chien anesthésié ou éveillé, l'action du produit (que celui-ci soit administré par voie intraveineuse ou par voie digestive) se traduit par une augmentation rapide et considérable de la quantité d'insuline sécrétée par le pancréas. Cette action se prolonge pendant plusieurs heures.In vitro l'action directe du produit sur le pancréas a été démontrée sur le pancréas isolé et perfusé du rat, même à très faibles concentrations. — Chez la souris le RP 22410 administré chroniquementper os stimule la néogénèse des îlots de Langerhans et des cellules bêta. Il est donc doué de l'action bêtacytotrophe.
    Abstract: Zusammenfassung Glisoxepid oder RP 22410 ist ein neuer, stark aktiver, blutzuckersenkender Sulfonylharnstoff. Je nachdem ob die Dosen in Gewichten oder Mol ausgedrückt werden, ist er am wachen Hund bei intravenöser Applikation 81 bzw. 131mal aktiver als Tolbutamid. Die blutzuckersenkende Wirkung zeigt sich nicht am vollständig pankreatektomierten Hund. -Diese Substanz stimuliert die Insulinsekretion.In vivo zeigt sich ihre Wirkung am anästhesierten oder wachen Hund in einer schnellen und beträchtlichen Erhöhung der vom Pankreas sezernierten Insulinmenge unabhängig davon ob sie intravenös oderper os verabreicht wird. Diese Wirkung bleibt über mehrere Stunden bestehen.In vitro wurde die direkte Wirkung der Substanz auf den isolierten und perfundierten Pankreas der Ratte auch in sehr geringen Konzentrationen nachgewiesen. -Bei der Maus stimuliert RP 22410 bei chronischer Verabreichungper os die Neubildung von Langerhansschen Inseln und B-Zellen. Sie besitzt daher eine betacytotrophe Wirkung.
    Notes: Summary Glisoxepid or RP 22410 is a new very active hypoglycaemic sulphonylurea. In the normal conscious dog, RP 22410 administered intravenously was 81 or 131 times more active than tolbutamide, depending on whether the dose is expressed in grams or in moles. The hypoglycaemic effect did not occur in the totally pancreatectomized dog. — RP 22410 stimulated insulin secretion.In vivo in the anaesthetized or conscious dog, the action of the drug (whether it be administered intravenously or orally) resulted in a rapid and considerable increase of the amount of insulin secreted by the pancreas. This action lasted several hours.In vitro the direct action of the product on the pancreas was demonstrated on the isolated and perfused rat pancreas, even at very low concentrations. — In the mouse, prolonged oral administration of RP 22410 stimulated neogenesis of the islets of Langerhans and of the beta cells. It therefore possesses betacytotrophic action.
    Type of Medium: Electronic Resource
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  • 2
    ISSN: 1432-0428
    Keywords: Glibenclamide ; hypoglycaemic sulphonamide ; oral antidiabetic substances ; islets of Langerhans ; islet development ; beta cells ; betacytotrophic action ; insulin secretion ; insulin synthesis ; diabetes prevention
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Description / Table of Contents: Résumé Les auteurs ont montré chez la souris que le HB 419 administré chroniquement, stimule le développement des îlots de Langerhans et des cellules bêta. Ce produit est donc doué de l'≪action bêtacytotrophe. Chez le chien normal, l'administration pendant 4 mois de HB 419 a pour effets d'abaisser la glycémie à jeun ainsi que l'ensemble de la courbe de la glycémie nycthémérale.- L'expérimentation effectuée montre que sous l'influence de l'administration prolongée de HB 419, la quantité d'insuline endogène synthétisée et sécrétée en plus de la sécrétion normale est considérable.
    Abstract: Zusammenfassung Die Autoren zeigten an Mäusen, daß chronische Gaben von HB 419 die Entwicklung der Langerhans'schen Inseln und der B-Zellen fördern. Die Substanz besitzt also eine betacytotrophe Wirkung“.Bei normalen Hunden bewirkt Zufuhr von HB 419 über 4 Monate eine Senkung der Nüchternblutzucker-Werte und der 24 Std-Blutzuckerkurven. Unter den gewählten Versuchsbedingungen konnte demonstriert werden, daß es unter dem Einfluß einer Dauerzufuhr von HB 419 zu einer erheblichen Mehrproduktion und Mehrfreisetzung von endogenem Insulin kommt.
    Notes: Summary The authors have demonstrated that HB 419 chronically administered in the mouse, stimulated the development of the islets of Langerhans and particularly that of the beta cells. This substance is thus endowed with a “beta cytotrophic” action. — In the normal dog, HB 419 administered over a four-month period resulted in a decreased fasting glycaemia, as well as a decrease of the entire nyctohemeral glycaemia curve. The experiments carried out showed that under the influence of prolonged HB 419 administration, the amount of endogenous insulin synthesized and secreted over and above the normal secretory level, was considerable.
    Type of Medium: Electronic Resource
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  • 3
    ISSN: 1432-0428
    Keywords: Beta cell ; isolated pancreas ; insulin secretion ; acetylcholine ; eserine ; cholinergic receptors ; muscarinic receptors ; atropine ; muscarine
    Source: Springer Online Journal Archives 1860-2000
    Topics: Medicine
    Notes: Summary Studies of the role and nature of the cholinergic receptors acting on the secretion of isolated perfused rat pancreas have shown the following: The infusion of acetylcholine at a dose of 2.5 μM in the presence of a concentration of glucose of 1.5 g/1, provoked a first phase of immediate and important stimulation of the secretion of insulin; this initial peak of insulin secretion was followed by a second phase during which a new less intense stimulation occurred; the latter was followed by an inhibition appearing at a time that depended on the pancreas used. At a dose of 0.5 μM of acetylcholine, the first phase of stimulation always appeared; during the second phase some pancreases were inhibited, others remained stimulated. — The peak of insulin secretion obtained by stimulation with acetylcholine during the first phase was dose related. — Eserine intensified the effects of acetylcholine. — The presence of glucose was essential for the insulinsecretory action of acetylcholine. The muscarinic nature of the cholinergic receptors implicated in the secretion of insulin was demonstrated by the use of: — Atropine which completely blocked the effects of acetylcholine, — Muscarine which produced the same effects as acetylcholine on our pancreas preparation, effects which were equally inhibited by atropine. The cholinergic receptors of the endocrine beta cell of the islet of Langerhans of the pancreas are therefore of the muscarinic type.
    Type of Medium: Electronic Resource
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  • 4
    ISSN: 1432-1041
    Keywords: Carbamazepine ; Saliva ; Mania ; Carbamazepine epoxide ; drug concentration ; Concentration-response relationship ; therapeutic monitoring
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The study was designed to investigate the antimanic profile of carbamazepine as a first-line drug in affective or schizoaffective disorders, to correlate the clinical efficacy with the plasma level of carbamazepine and its 10,11-epoxide metabolite, and to test the potential value of monitoring the salivary level. It was administered alone for 3 weeks to 21 acute manic inpatients. During the first week, the dosage was rapidly increased to 800 mg/day in order to produce steady-state plasma levels of carbamazepine on Day 7. The individual dose was then adjusted to maintain the therapeutic range of 8–12 mg/l. Plasma and saliva levels of the drug and its metabolite, as well as clinical status were assessed weekly. Overall, there was 62% globally improved patients and 77% in affective disorders. The improvement of manic symptoms was significantly lower in schizoaffective than in affective disorders, whereas the dropout rate and the need for antipsychotic medication was higher in the former group. The antimanic response was significantly correlated with the plasma levels both of carbamazepine and its epoxide metabolite, with a time-lag consistent with a delayed drug effect. Drug and metabolite concentrations in saliva were close to their plasma free fraction and were strongly correlated with their plasma levels, suggesting the potential value of salivary drug monitoring.
    Type of Medium: Electronic Resource
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  • 5
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 224 (1981), S. 289-299 
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 6
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 375 (1986), S. 101-110 
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 7
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 307 (1984), S. 351-359 
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 8
    Electronic Resource
    Electronic Resource
    Amsterdam : Elsevier
    Journal of Chromatography B: Biomedical Sciences and Applications 572 (1991), S. 269-276 
    ISSN: 0378-4347
    Source: Elsevier Journal Backfiles on ScienceDirect 1907 - 2002
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
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  • 9
    Electronic Resource
    Electronic Resource
    Oxford, UK : Blackwell Publishing Ltd
    Annals of the New York Academy of Sciences 150 (1968), S. 0 
    ISSN: 1749-6632
    Source: Blackwell Publishing Journal Backfiles 1879-2005
    Topics: Natural Sciences in General
    Type of Medium: Electronic Resource
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