Protection and reversal of excitotoxic neuronal damage by glucagon-like peptide-1 and exendin-4

J Pharmacol Exp Ther. 2002 Sep;302(3):881-8. doi: 10.1124/jpet.102.037481.

Abstract

Glucagon-like peptide-1 (7-36)-amide (GLP-1) is an endogenous insulinotropic peptide that is secreted from the L cells of the gastrointestinal tract in response to food. It has potent effects on glucose-dependent insulin secretion, insulin gene expression, and pancreatic islet cell formation. In type 2 diabetes, GLP-1, by continuous infusion, can normalize blood glucose and is presently being tested in clinical trials as a therapy for this disease. More recently, GLP-1 has been found to have central nervous system (CNS) effects and to stimulate neurite outgrowth in cultured cells. We now report that GLP-1, and its longer-acting analog exendin-4, can completely protect cultured rat hippocampal neurons against glutamate-induced apoptosis. Extrapolating these effects to a well defined rodent model of neurodegeneration, GLP-1 and exendin-4 greatly reduced ibotenic acid-induced depletion of choline acetyltransferase immunoreactivity in basal forebrain cholinergic neurons. These findings identify a novel neuroprotective/neurotrophic function of GLP-1 and suggest that such peptides may have potential for halting or reversing neurodegenerative processes in CNS disorders, such as Alzheimer's disease, and in neuropathies associated with type 2 diabetes mellitus.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Basal Ganglia / pathology
  • Cell Death / drug effects
  • Cell Survival / drug effects
  • Cells, Cultured
  • Choline O-Acetyltransferase / metabolism
  • Cyclic AMP / metabolism
  • Excitatory Amino Acid Agonists / toxicity
  • Excitatory Amino Acid Antagonists / toxicity*
  • Exenatide
  • Glial Fibrillary Acidic Protein / metabolism
  • Glucagon / metabolism
  • Glucagon / pharmacology*
  • Glucagon-Like Peptide 1
  • Glucagon-Like Peptide-1 Receptor
  • Glutamic Acid / toxicity*
  • Hippocampus / cytology
  • Hippocampus / drug effects
  • Ibotenic Acid / antagonists & inhibitors
  • Ibotenic Acid / toxicity
  • Immunohistochemistry
  • Nerve Degeneration / chemically induced*
  • Nerve Degeneration / prevention & control*
  • Neurons / drug effects*
  • Neurons / pathology
  • Parasympathetic Nervous System / drug effects
  • Peptide Fragments / metabolism
  • Peptide Fragments / pharmacology*
  • Peptides / pharmacology*
  • Protein Precursors / metabolism
  • Protein Precursors / pharmacology*
  • Rats
  • Rats, Inbred F344
  • Rats, Sprague-Dawley
  • Receptors, Glucagon / drug effects
  • Receptors, Glucagon / metabolism
  • Venoms*

Substances

  • Excitatory Amino Acid Agonists
  • Excitatory Amino Acid Antagonists
  • Glial Fibrillary Acidic Protein
  • Glp1r protein, rat
  • Glucagon-Like Peptide-1 Receptor
  • Peptide Fragments
  • Peptides
  • Protein Precursors
  • Receptors, Glucagon
  • Venoms
  • Ibotenic Acid
  • Glutamic Acid
  • Glucagon-Like Peptide 1
  • Glucagon
  • Exenatide
  • Cyclic AMP
  • Choline O-Acetyltransferase