Delta-opioid agonist SNC-121 protects retinal ganglion cell function in a chronic ocular hypertensive rat model

Invest Ophthalmol Vis Sci. 2013 Mar 11;54(3):1816-28. doi: 10.1167/iovs.12-10741.

Abstract

Purpose: This study examined if the delta-opioid (δ-opioid) receptor agonist, SNC-121, can improve retinal function and retinal ganglion cell (RGC) survival during glaucomatous injury in a chronic ocular hypertensive rat model.

Methods: IOP was raised in brown Norway rats by injecting hypertonic saline into the limbal venous system. Rats were treated with 1 mg/kg SNC-121 (intraperitoneally [IP]) once daily for 7 days. Pattern-electroretinograms (PERGs) were obtained in response to contrast reversal of patterned visual stimuli. RGCs were visualized by fluorogold retrograde labeling. Expression of TNF-α and p38 mitogen-activated protein (MAP) kinase was measured by immunohistochemistry and Western blotting.

Results: PERG amplitudes in ocular hypertensive eyes were significantly reduced (14.3 ± 0.60 μvolts) when compared with healthy eyes (18.0 ± 0.62 μvolts). PERG loss in hypertensive eyes was inhibited by SNC-121 treatment (17.20 ± 0.1.3 μvolts; P < 0.05). There was a 29% loss of RGCs in the ocular hypertensive eye, which was inhibited in the presence of SNC-121. TNF-α production and activation of p38 MAP kinase in retinal sections and optic nerve samples were upregulated in ocular hypertensive eyes and inhibited in the presence of SNC-121. Furthermore, TNF-α induced increase in p38 MAP kinase activation in astrocytes was inhibited in the presence of SNC-121.

Conclusions: These data provide evidence that activation of δ-opioid receptors inhibited the loss of PERG amplitudes and rate of RGC loss during glaucomatous injury. Mechanistic data provided clues that TNF-α is mainly produced from glial cells and activates p38 MAP kinase, which was significantly inhibited by SNC-121 treatment. Overall, data indicate that enhancement of δ-opioidergic activity in the eye may provide retina neuroprotection against glaucoma.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Astrocytes / metabolism
  • Benzamides / therapeutic use*
  • Blotting, Western
  • Cell Survival / drug effects
  • Chronic Disease
  • Cytoprotection
  • Disease Models, Animal*
  • Electroretinography
  • Female
  • Immunohistochemistry
  • Injections, Intraperitoneal
  • Intraocular Pressure / physiology
  • Male
  • Neuroprotective Agents / therapeutic use*
  • Ocular Hypertension / metabolism
  • Ocular Hypertension / physiopathology
  • Ocular Hypertension / prevention & control*
  • Optic Disk / cytology
  • Piperazines / therapeutic use*
  • Rats
  • Rats, Inbred BN
  • Receptors, Opioid, delta / agonists*
  • Retina / physiopathology
  • Retinal Ganglion Cells / physiology*
  • Tumor Necrosis Factor-alpha / metabolism
  • p38 Mitogen-Activated Protein Kinases / metabolism

Substances

  • Benzamides
  • Neuroprotective Agents
  • Piperazines
  • Receptors, Opioid, delta
  • Tumor Necrosis Factor-alpha
  • SNC 121
  • p38 Mitogen-Activated Protein Kinases