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Published on: May 10, 2018

Mosapride, a 5HT-4 receptor agonist, improves insulin sensitivity and glycaemic control in patients with Type II

N Ueno1, A Inui, A Asakawa

  • 1Division of Diabetes, Digestive and Kidney Diseases, Department of Clinical Molecular Medicine, Kobe University Graduate School of Medicine, 7-5-1 Kusunoki-cho, Chuo-ku, Kobe 650-0017, Japan.

Diabetologia
|July 11, 2002
PubMed
Abstract

Insights

Mosapride, a 5HT-4 receptor agonist, improved glycemic control in Type II diabetes patients by enhancing insulin action in muscles. This study shows potential for mosapride in managing blood sugar levels.

Area of Science:

  • Endocrinology
  • Pharmacology

Background:

  • Type II diabetes mellitus (T2DM) is a metabolic disorder characterized by insulin resistance and impaired glucose metabolism.
  • Effective glycemic control is crucial in managing T2DM and preventing long-term complications.
  • 5HT-4 receptor agonists are being explored for their potential therapeutic effects beyond gastrointestinal motility.

Purpose of the Study:

  • To investigate the efficacy of mosapride, a selective 5HT-4 receptor agonist, in improving glycemic control in patients with Type II diabetes mellitus.
  • To assess the impact of mosapride on insulin sensitivity and insulin receptor function in diabetic patients without autonomic neuropathy.

Main Methods:

  • Two studies were conducted: a 1-week inpatient study (n=34) and an 8-week outpatient study (n=69) with Type II diabetes patients.
  • Participants received either mosapride (5 mg TID) or a placebo.
  • Methods included blood glucose and insulin level measurements, intravenous glucose loading, hyperinsulinemic-normoglycemic clamp studies, insulin receptor analysis on erythrocytes, and RT-PCR for 5HT-4 receptor expression.

Main Results:

  • Mosapride significantly reduced fasting blood glucose and fructosamine levels in the short-term study.
  • It enhanced insulin receptor number and autophosphorylation, and increased glucose utilization in patients.
  • The 8-week treatment led to significant reductions in fasting glucose, insulin, and HbA1c levels.
  • RT-PCR confirmed 5HT-4 receptor expression predominantly in muscle tissue.

Conclusions:

  • Mosapride demonstrates a beneficial effect on glycemic control in Type II diabetic patients.
  • The drug appears to improve insulin action, particularly at the muscle level.
  • Mosapride holds potential as an adjunct therapy for managing Type II diabetes mellitus.

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