Pharmacological and functional characterization of endothelin receptors in bovine trabecular meshwork and ciliary muscle

Ophthalmic Res. 2005 Jul-Aug;37(4):179-87. doi: 10.1159/000086471. Epub 2005 Jun 21.

Abstract

To clarify the potential role of endothelin-1 (ET-1) in the pathogenesis of glaucoma, the endothelin receptors expressed in bovine trabecular meshwork (TM) and ciliary muscle (CM) were identified. TM and CM strips were subjected to ET-1 as well as to specific endothelin receptor antagonists. In both tissues BQ123, a specific ET-A receptor antagonist, substantially inhibited ET-1-induced contraction. BQ788, a specific ET-B receptor antagonist, showed only moderate effects. Both ET receptor types were detected in bovine TM and CM using Western blot analysis. ET-1 produced an increase in intracellular calcium in cultured TM cells. This effect was inhibited by BQ123, but not by BQ788. Thus, although both receptors are present, the ET-A receptor appears to play the predominant role in mediating contraction in both the TM and CM, while the ET-B receptor seems to contribute little to the overall ET-1 effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blotting, Western
  • Calcium / metabolism
  • Cattle
  • Cells, Cultured
  • Ciliary Body / drug effects*
  • Ciliary Body / metabolism
  • Endothelin A Receptor Antagonists
  • Endothelin B Receptor Antagonists
  • Endothelin-1 / pharmacology*
  • Muscle Contraction / physiology
  • Muscle, Smooth / drug effects*
  • Muscle, Smooth / metabolism
  • Oligopeptides / pharmacology
  • Peptides, Cyclic / pharmacology
  • Piperidines / pharmacology
  • Receptor, Endothelin A / physiology*
  • Receptor, Endothelin B / physiology*
  • Trabecular Meshwork / drug effects
  • Trabecular Meshwork / metabolism

Substances

  • Endothelin A Receptor Antagonists
  • Endothelin B Receptor Antagonists
  • Endothelin-1
  • Oligopeptides
  • Peptides, Cyclic
  • Piperidines
  • Receptor, Endothelin A
  • Receptor, Endothelin B
  • BQ 788
  • cyclo(Trp-Asp-Pro-Val-Leu)
  • Calcium