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The effect of mosapride (5HT-4 receptor agonist) on insulin sensitivity and GLUT4 translocation

J S Nam1, J Y Nam, J S Yoo

  • 1Department of Internal Medicine, Yonsei University College of Medicine, Seoul, Republic of Korea.

Diabetes Research and Clinical Practice
|January 12, 2010
PubMed
Abstract

Insights

Mosapride effectively lowers fasting blood glucose in individuals with impaired glucose tolerance by enhancing glucose transporter type 4 (GLUT4) translocation in muscles, without increasing insulin secretion.

Area of Science:

  • Metabolic disorders
  • Pharmacology
  • Endocrinology

Background:

  • Impaired glucose tolerance (IGT) is a precursor to type 2 diabetes.
  • Understanding novel therapeutic targets for glucose control is crucial.

Purpose of the Study:

  • To investigate the effect of mosapride, a 5HT-4 agonist, on blood glucose and insulin sensitivity in IGT subjects.
  • To elucidate the in vitro mechanism of action of mosapride on glucose metabolism.

Main Methods:

  • A 2-week randomized, placebo-controlled trial in 30 IGT patients.
  • Assessment of biochemical profiles and insulin sensitivity via euglycemic hyperinsulinemic clamp.
  • In vitro study on human skeletal muscle cells to evaluate GLUT4 translocation and IRS-1 phosphorylation.

Main Results:

  • Mosapride significantly increased glucose disposal rates and decreased fasting plasma glucose and insulin levels.
  • Mosapride enhanced GLUT4 translocation to the plasma membrane in skeletal muscle cells.
  • Mosapride did not affect tyrosine phosphorylation of IRS-1, unlike insulin.

Conclusions:

  • Mosapride demonstrates efficacy in reducing fasting glucose in IGT patients.
  • The glucose-lowering effect may be attributed to increased GLUT4 translocation in skeletal muscles.
  • Mosapride offers a potential therapeutic strategy for managing IGT without stimulating insulin secretion.

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