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English Journal
- Effect of linagliptin, alone and in combination with voglibose or exendin-4, on glucose control in male ZDF rats.
- Jones RB1, Vickers SP1, Cheetham SC2, Headland KR1, Mark M3, Klein T3.Author information 1RenaSci Limited, BioCity, Pennyfoot Street, Nottingham NG1 1GF, UK.2RenaSci Limited, BioCity, Pennyfoot Street, Nottingham NG1 1GF, UK. Electronic address: sharon.cheetham@renasci.co.uk.3Boehringer Ingelheim Pharma GmbH & Co. KG, Biberach an der Riss, Germany.AbstractThe effects of the dipeptidyl peptidase-4 (DPP-4) inhibitor, linagliptin, alone and in combination with voglibose or exendin-4, on glycaemic control and body weight were assessed in an animal model of type 2 diabetes. Voglibose is an α-glucosidase inhibitor but also increases glucagon-like peptide 1 (GLP-1). Exendin-4 is a GLP-1 receptor agonist. Male Zucker Diabetic Fatty (ZDF) rats were dosed for 3 days, fasted overnight and a sucrose/glucose tolerance test was performed. Linagliptin (1mg/kg po) improved glucose tolerance by increasing plasma GLP-1 (active) and insulin secretion, whilst having no effect on body weight. Voglibose (1 and 10mg/kg po) reduced body weight, improved glycaemic control, reduced plasma insulin and increased total but not active GLP-1. The combination of linagliptin and voglibose significantly reduced body weight, improved glycaemic control and reduced plasma insulin compared to linagliptin alone. Furthermore, linagliptin plus voglibose produced a marked increase in GLP-1 (active) at 5min post-sucrose, compared to linagliptin, possibly because linagliptin prevented the degradation of GLP-1 secreted in response to voglibose. Exendin-4 (10μg/kg sc) significantly reduced body weight, improved glucose tolerance but reduced GLP-1 (active). The combination of linagliptin and exendin-4 significantly reduced body weight and improved glycaemic control but had no effect on plasma GLP-1. Overall it did not markedly improve glycaemic control compared to the individual drugs. The improved glucose control, reduced body weight and markedly increased plasma GLP-1 levels in animals given linagliptin with voglibose, suggests that this combination may be particularly beneficial in the treatment of type 2 diabetes.
- European journal of pharmacology.Eur J Pharmacol.2014 Apr 15;729:59-66. doi: 10.1016/j.ejphar.2014.02.004. Epub 2014 Feb 14.
- The effects of the dipeptidyl peptidase-4 (DPP-4) inhibitor, linagliptin, alone and in combination with voglibose or exendin-4, on glycaemic control and body weight were assessed in an animal model of type 2 diabetes. Voglibose is an α-glucosidase inhibitor but also increases glucagon-like peptide
- PMID 24530555
- Chronic treatment with the dipeptidyl peptidase-4 inhibitor BI 1356 [(R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione] increases basal glucagon-like peptide-1 and improves glycemic control in diabetic rodent models.
- Thomas L1, Tadayyon M, Mark M.Author information 1Boehringer Ingelheim Pharma GmbH and Co. KG, Department of Metabolic Diseases Research, Birkendorfer Strasse 65, D-88397 Biberach an der Riss, Germany. leo.thomas@boehringer-ingelheim.comAbstractAntidiabetic effects of dipeptidyl peptidase-4 (DPP-4) inhibitors are exerted by potentiation of the biological activity of incretin hormones like glucagon-like peptide (GLP)-1. BI 1356 [proposed trade name Ondero; (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione] is a novel competitive, selective, potent, and long-acting DPP-4 inhibitor under clinical development for the treatment of type 2 diabetes. The effect of 1 to 2 months of chronic dosing of BI 1356 in two different animal models was investigated. The first is a primarily genetic model (Zucker diabetic fatty rats), and the second is a nongenetic model (mice with diabetes induced by a combination of high-fat diet and low-dose streptozotocin). BI 1356 was shown to lower HbA1c after multiple dosing in both models. The improvement of glycemic control achieved in disease models of different etiology suggests that BI 1356 would also be efficacious in treating a broad spectrum of type 2 diabetic patients. In addition, multiple dosing of BI 1356 leads to a sustained increase in basal levels of active GLP-1 in the systemic circulation, with expected long-term benefits on pancreatic alpha- and beta-cells. The effects on HbA1c and GLP-1 were superior to the short-acting DPP-4 inhibitor vildagliptin, demonstrating the potential of BI 1356 as a once daily treatment for type 2 diabetes at low therapeutic doses.
- The Journal of pharmacology and experimental therapeutics.J Pharmacol Exp Ther.2009 Feb;328(2):556-63. doi: 10.1124/jpet.108.143966. Epub 2008 Oct 29.
- Antidiabetic effects of dipeptidyl peptidase-4 (DPP-4) inhibitors are exerted by potentiation of the biological activity of incretin hormones like glucagon-like peptide (GLP)-1. BI 1356 [proposed trade name Ondero; (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethy
- PMID 18971371
- [Air microorganisms in animal housing--4. Airborne gram-negative bacteria and airborne endotoxin in pig houses].
- Zucker BA1, Müller W.Author information 1Institut für Tier- und Umwelthygiene der Freien Universität Berlin.AbstractThe species composition of airborne gram-negative bacteria and the relationship between inhalable endotoxin, inhalable dust and airborne bacteria were studied in 4 pig houses. The airborne gram-negative bacterial flora was dominated by Enterobacteriaceae. Within the Enterobacteriaceae the species E. coli and Enterobacter agglomerans were predominant. Significant correlation were found between the concentration of inhalable dust and inhalable endotoxin as well as between the concentration of airborne gram-negative bacteria and inhalable endotoxin. However these correlation were not very strong. With respect to the characterization of the potential hazard of organic dust exposure, measurements of the concentration of airborne dust or airborne bacteria should not be used for the estimation of the concentration of airborne endotoxin.
- Berliner und Münchener tierärztliche Wochenschrift.Berl Munch Tierarztl Wochenschr.2002 Jan-Feb;115(1-2):30-6.
- The species composition of airborne gram-negative bacteria and the relationship between inhalable endotoxin, inhalable dust and airborne bacteria were studied in 4 pig houses. The airborne gram-negative bacterial flora was dominated by Enterobacteriaceae. Within the Enterobacteriaceae the species E.
- PMID 11852681
Japanese Journal
- Vorsorgeuntersuchung für Säuglinge and Kleinkinder im entlegenen Landkreis vor allem Häufigkeit der angeborenen Erkrankungen and der behinderten Kinder
- 柳沢 文憲
- 民族衛生 36(4), 130-137, 1970
- … Im Landkreis wird Vorsorgeuntersuchung für Säuglinge and Kleinkinder noch nicht genügend aüsgef uhrt, obwohl die Vorsorgeuntersuchung der Säuglinge and 3-jährigen Kinder in Japan durch den Gesundheitsamt seit etwa 10 Jahren eingeführt wird. … Urinuntersuchung : Eiweiß, Zucker u. … Das Prozentsatz der Untersuchung unter 5. … Im allgemeinen findet sich gute Gesundheitspflege der Kinder trotz des entlegenen Landes. …
- NAID 130002026701
- Polyamino-Zucker. VI. Synthese von Derivaten der 2,3,4-Triamino-2,3,4-tridesoxy-β-D-glucose
- Nakagawa Toshio,Sato Yoshikuni,Takamoto Tetsuyoshi,Lichtenthaler Frieder W.,Majer Norbert
- Bulletin of the Chemical Society of Japan 43(12), 3866-3869, 1970
- A facile synthesis of methyl and phenyl glycoside derivatives of 2,3,4-triamino-2,3,4-trideoxy-β-D-glucopyranose is described, involving as the integral part the diamination with benzylamine or ammoni …
- NAID 130001977414
- Klinische Untersuchungen Über Brenztraubensäurestoffwechsel bei den Leberkrankheiten Ⅱ. Mitteilung: Einflüsse der verschiedenen Medikamente auf den Brenztraubensäureblutspiegel bei den Leberkrankheiten
- Kono Hiroshi
- Acta Medicinae Okayama 18(2), 1964-04
- … <p>Sowohl aus dem Grunde, den Mechanismus des gestörten BTS-Stoffwechsels bei den Leberkrankheiten zu erkennen, als auch Beobachtungen für seine Behandlungen zu machen, wurden die Ein£liisse von Zucker, Thiamin und seinen Derivaten (BTMP, TTFD), Thioctsäure, der Verbindung zwischen dem Derivat von Thiamin und Thioctsaure (TATD), Kalium- und Magnesium-Asparaginat und Glucocorticoiden auf den BTS-Blutspiegel untersucht. …
- NAID 120002312074
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