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Chemical Compound Review

Glufast     4-(1,3,3a,4,5,6,7,7a- octahydroisoindol-2...

Synonyms: AC1MILSA, AC1NUHLY, CHEMBL471498, SureCN676865, Kad-1229, ...
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Disease relevance of Mitiglinide


High impact information on Mitiglinide


Biological context of Mitiglinide


Anatomical context of Mitiglinide

  • 6. Our results show that mitiglinide is a high-affinity drug that shows a 1000 fold greater affinity for the beta-cell type than the cardiac and smooth muscle types of K(ATP) channel, when measured in excised patches [8].
  • Effects of mitiglinide and sulfonylureas in isolated canine coronary arteries and perfused rat hearts [2].
  • These results indicate that, similar to the sulfonylureas, mitiglinide is highly specific to the Kir6.2/SUR1 complex, i.e., the pancreatic beta-cell K(ATP) channel, and suggest that mitiglinide may be a clinically useful anti-diabetic drug [9].
  • In contrast, as in the 12-wk-old rats, a precipitous rise in insulin secretion was seen in the portal vein of 24-wk-old rats given mitiglinide, which peaked 15 min after mitiglinide administration, but the insulin levels continued to increase for 120 min or longer in the 24-wk-old rats given glibenclamide [10].
  • They were also given mitiglinide orally and examined for LPL mRNA expression in their adipose tissue [10].

Associations of Mitiglinide with other chemical compounds


Gene context of Mitiglinide


Analytical, diagnostic and therapeutic context of Mitiglinide

  • Determination of mitiglinide in rat plasma by high-performance liquid chromatography with UV detection [4].
  • The patients who were well controlled with mitiglinide regimen were significantly younger (51.9 +/- 16.0 years, p<0.005) and heavier (body mass index: 25.7 +/- 3.3 kg/m(2), p<0.05) than those who were not (67.9 +/- 8.7 and 23.0 +/- 3.1, respectively) [3].


  1. Characterization of the action of S 21403 (mitiglinide) on insulin secretion and biosynthesis in normal and diabetic beta-cells. Kaiser, N., Nesher, R., Oprescu, A., Efendic, S., Cerasi, E. Br. J. Pharmacol. (2005) [Pubmed]
  2. Effects of mitiglinide and sulfonylureas in isolated canine coronary arteries and perfused rat hearts. Maruyama, I., Tomiyama, Y., Maruyama, K., Ojima, K., Kobayashi, K., Kobayashi, M., Yamazaki, Y., Kojima, M., Shibata, N. Eur. J. Pharmacol. (2006) [Pubmed]
  3. Therapeutic efficacy of mitiglinide combined with once daily insulin glargine after switching from multiple daily insulin regimen of aspart insulin and glargine in patients with type 2 diabetes mellitus. Yoshihara, T., Kumashiro, N., Kanazawa, Y., Mita, T., Sakurai, Y., Kawai, J., Abe, M., Motojima, K., Hara, K., Yamazaki, Y., Kanazawa, A., Miwa, S., Sato, F., Kanno, R., Shimizu, T., Sakai, K., Uchino, H., Watada, H., Tanaka, Y., Kawamori, R., Hirose, T. Endocr. J. (2006) [Pubmed]
  4. Determination of mitiglinide in rat plasma by high-performance liquid chromatography with UV detection. Lushan, Y., Su, Z. J. Chromatogr. B Analyt. Technol. Biomed. Life Sci. (2006) [Pubmed]
  5. Study of the insulinotropic effect of the novel antihyperglycemic agent KAD-1229 using HIT T15 cells, a hamster's insulinoma cell line. Ichikawa, K., Yamato, T., Tsuji, A., Ojima, K., Kusama, H., Kojima, M. Arzneimittel-Forschung. (2002) [Pubmed]
  6. Imaging docking and fusion of insulin granules induced by antidiabetes agents: sulfonylurea and glinide drugs preferentially mediate the fusion of newcomer, but not previously docked, insulin granules. Nagamatsu, S., Ohara-Imaizumi, M., Nakamichi, Y., Kikuta, T., Nishiwaki, C. Diabetes (2006) [Pubmed]
  7. Effects of S21403 (mitiglinide) on postprandial generation of oxidative stress and inflammation in type 2 diabetic patients. Assaloni, R., Da Ros, R., Quagliaro, L., Piconi, L., Maier, A., Zuodar, G., Motz, E., Ceriello, A. Diabetologia (2005) [Pubmed]
  8. Effects of mitiglinide (S 21403) on Kir6.2/SUR1, Kir6.2/SUR2A and Kir6.2/SUR2B types of ATP-sensitive potassium channel. Reimann, F., Proks, P., Ashcroft, F.M. Br. J. Pharmacol. (2001) [Pubmed]
  9. The effects of mitiglinide (KAD-1229), a new anti-diabetic drug, on ATP-sensitive K+ channels and insulin secretion: comparison with the sulfonylureas and nateglinide. Sunaga, Y., Gonoi, T., Shibasaki, T., Ichikawa, K., Kusama, H., Yano, H., Seino, S. Eur. J. Pharmacol. (2001) [Pubmed]
  10. Effects of mitiglinide on glucose-induced insulin release into the portal vein and fat-induced triglyceride elevation in prediabetic and diabetic OLETF rats. Mori, Y., Ojima, K., Fuujimori, Y., Fujimori, Y., Aoyagi, I., Kusama, H., Yamazaki, Y., Kojima, M., Kojima, S., Shibata, N., Itoh, Y., Tajima, N. Endocrine (2006) [Pubmed]
  11. Inhibition of heterologously expressed cystic fibrosis transmembrane conductance regulator Cl- channels by non-sulphonylurea hypoglycaemic agents. Cai, Z., Lansdell, K.A., Sheppard, D.N. Br. J. Pharmacol. (1999) [Pubmed]
  12. Long-term Effect of Combination Therapy with Mitiglinide and Once Daily Insulin Glargine in Patients who were Successfully Switched from Intensive Insulin Therapy in Short-term Study. Kumashiro, N., Yoshihara, T., Kanazawa, Y., Shimizu, T., Watada, H., Tanaka, Y., Fujitani, Y., Kawamori, R., Hirose, T. Endocr. J. (2007) [Pubmed]
  13. Recent developments and emerging therapies for type 2 diabetes mellitus. Evans, A.J., Krentz, A.J. Drugs in R&D. (1999) [Pubmed]
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