Comparison of Efficacies of a Dipeptidyl Peptidase IV Inhibitor and .ALPHA.-Glucosidase Inhibitors in Oral Carbohydrate and Meal Tolerance Tests and the Effects of Their Combination in Mice
-
- Yamazaki Kazuto
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
-
- Inoue Takashi
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
-
- Yasuda Nobuyuki
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
-
- Sato Yoshiaki
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
-
- Nagakura Tadashi
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
-
- Takenaka Osamu
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
-
- Clark Richard
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
-
- Saeki Takao
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
-
- Tanaka Isao
- Tsukuba Research Laboratories, Eisai Co., Ltd., Japan
Bibliographic Information
- Other Title
-
- Comparison of efficacies of a dipeptidyl peptidase 4 inhibitor and α-glucosidase inhibitors in oral carbohydrate and meal tolerance tests and the effects of their combination in mice
- Comparison of efficacies of a dipeptidyl peptidase 4 inhibitor and a glucosidase inhibitors in oral carbohydrate and meal tolerance tests and the effects of their combination in mice
- Comparison of Efficacies of a Dipeptidyl Peptidase IV Inhibitor and α-Glucosidase Inhibitors in Oral Carbohydrate and Meal Tolerance Tests and the Effects of Their Combination in Mice
Search this article
Description
E3024 (3-but-2-ynyl-5-methyl-2-piperazin-1-yl-3,5-dihydro-4H-imidazo[4,5-d]pyridazin-4-one tosylate) is a dipeptidyl peptidase IV (DPP-IV) inhibitor. Since the target of both DPP-IV inhibitors and α-glucosidase inhibitors is the lowering of postprandial hyperglycemia, we compared antihyperglycemic effects for E3024 and α-glucosidase inhibitors in various oral carbohydrate and meal tolerance tests using normal mice. In addition, we investigated the combination effects of E3024 and voglibose on blood glucose levels in a meal tolerance test using mice fed a high-fat diet. ER-235516-15 (the trifluoroacetate salt form of E3024, 1 mg/kg) lowered glucose excursions consistently, regardless of the kind of carbohydrate loaded. However, the efficacy of acarbose (10 mg/kg) and of voglibose (0.1 mg/kg) varied with the type of carbohydrate administered. The combination of E3024 (3 mg/kg) and voglibose (0.3 mg/kg) improved glucose tolerance additively, with the highest plasma active glucagon-like peptide-1 levels. This study shows that compared to α-glucosidase inhibitors, DPP-IV inhibitors may have more consistent efficacy to reduce postprandial hyperglycemia, independent of the types of carbohydrate contained in a meal, and that the combination of a DPP-IV inhibitor and an α-glucosidase inhibitor is expected to be a promising option for lowering postprandial hyperglycemia.<br>
Journal
-
- Journal of Pharmacological Sciences
-
Journal of Pharmacological Sciences 104 (1), 29-38, 2007
The Japanese Pharmacological Society
- Tweet
Keywords
Details 詳細情報について
-
- CRID
- 1390001205175192192
-
- NII Article ID
- 10024313894
-
- NII Book ID
- AA11806667
-
- COI
- 1:CAS:528:DC%2BD2sXmt1Wrtrw%3D
-
- ISSN
- 13478648
- 13478613
-
- NDL BIB ID
- 8737590
-
- PubMed
- 17485917
-
- Text Lang
- en
-
- Data Source
-
- JaLC
- NDL Search
- Crossref
- PubMed
- CiNii Articles
-
- Abstract License Flag
- Disallowed