NMDAR antagonists for the treatment of diabetes mellitus-Current status and future directions

Diabetes Obes Metab. 2017 Sep:19 Suppl 1:95-106. doi: 10.1111/dom.13017.

Abstract

Diabetes mellitus is characterized by chronically elevated blood glucose levels accelerated by a progressive decline of insulin-producing β-cells in the pancreatic islets. Although medications are available to transiently adjust blood glucose to normal levels, the effects of current drugs are limited when it comes to preservation of a critical mass of functional β-cells to sustainably maintain normoglycemia. In this review, we recapitulate recent evidence on the role of pancreatic N-methyl-D-aspartate receptors (NMDARs) in β-cell physiology, and summarize effects of morphinan-based NMDAR antagonists that are beneficial for insulin secretion, glucose tolerance and islet cell survival. We further discuss NMDAR-mediated molecular pathways relevant for neuronal cell survival, which may also be important for the preservation of β-cell function and mass. Finally, we summarize the literature for evidence on the role of NMDARs in the development of diabetic long-term complications, and highlight beneficial pharmacologic aspects of NMDAR antagonists in diabetic nephropathy, retinopathy as well as neuropathy.

Keywords: N-methyl-D-aspartate receptors (NMDARs); cardiovascular (CV) death; cell death; dextromethorphan (DXM); dextrorphan (DXO); diabetes mellitus; diabetic long-term complications; flow-mediated dilation (FMD); nephropathy; retinopathy.

Publication types

  • Review

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Diabetes Complications / prevention & control*
  • Diabetes Mellitus, Type 2 / complications
  • Diabetes Mellitus, Type 2 / drug therapy*
  • Diabetes Mellitus, Type 2 / metabolism
  • Diabetic Nephropathies / prevention & control
  • Diabetic Neuropathies / prevention & control
  • Diabetic Retinopathy / prevention & control
  • Drug Design
  • Drug Resistance, Multiple
  • Drugs, Investigational / adverse effects
  • Drugs, Investigational / chemistry
  • Drugs, Investigational / therapeutic use*
  • Glucagon / metabolism
  • Glucagon-Secreting Cells / drug effects
  • Glucagon-Secreting Cells / metabolism
  • Humans
  • Hyperglycemia / prevention & control*
  • Hypoglycemia / chemically induced
  • Hypoglycemia / prevention & control
  • Hypoglycemic Agents / adverse effects
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / therapeutic use*
  • Insulin / metabolism
  • Insulin Secretion
  • Insulin-Secreting Cells / drug effects*
  • Insulin-Secreting Cells / metabolism
  • Neuralgia / complications
  • Neuralgia / prevention & control
  • Receptors, N-Methyl-D-Aspartate / antagonists & inhibitors*
  • Receptors, N-Methyl-D-Aspartate / metabolism

Substances

  • Drugs, Investigational
  • Hypoglycemic Agents
  • Insulin
  • Receptors, N-Methyl-D-Aspartate
  • Glucagon