Effects of the serotonergic anxiolytic buspirone on plasma glucose and glucose-induced hyperglycemia in mice

J Pharmacol Sci. 2003 Dec;93(4):446-50. doi: 10.1254/jphs.93.446.

Abstract

Effects of the serotonergic anxiolytic buspirone on plasma glucose and glucose-induced hyperglycemia were studied in mice. Buspirone did not affect plasma glucose levels of non-fasted mice, while it increased serum insulin levels. In fasted mice, buspirone significantly reduced glucose-induced hyperglycemia and enhanced insulin release elicited by glucose. This suggests that buspirone enhances insulin release, resulting in inhibition of glucose-induced hyperglycemia. The major metabolite of buspirone, 1-(2-pyrimidinyl)piperazine (1-PP) increased serum insulin levels and induced a slight hypoglycemia in non-fasted mice. 1-PP decreases glucose-induced hyperglycemia and amplifies insulin release elicited by glucose in fasted mice. Since buspirone is mainly metabolized to 1-PP and formation of 1-PP occurs quickly, the inhibitory effect of buspirone on glucose-induced hyperglycemia is likely mediated by 1-PP.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Anxiety Agents / metabolism
  • Anti-Anxiety Agents / pharmacology*
  • Blood Glucose / drug effects*
  • Buspirone / analogs & derivatives*
  • Buspirone / metabolism
  • Buspirone / pharmacology*
  • Fasting
  • Glucose
  • Hyperglycemia / blood*
  • Hyperglycemia / chemically induced
  • Hyperglycemia / prevention & control
  • Hyperinsulinism / prevention & control
  • Injections, Subcutaneous
  • Insulin / blood
  • Insulin / metabolism
  • Insulin Secretion
  • Male
  • Mice
  • Serotonin Receptor Agonists / metabolism
  • Serotonin Receptor Agonists / pharmacology*
  • Time Factors

Substances

  • Anti-Anxiety Agents
  • Blood Glucose
  • Insulin
  • Serotonin Receptor Agonists
  • 1-(2-pyrimidinyl)piperazine
  • Glucose
  • Buspirone