ETA and ETB receptors on single smooth muscle cells cooperate in mediating guinea pig tracheal contraction

Am J Physiol. 1994 Feb;266(2 Pt 1):L113-24. doi: 10.1152/ajplung.1994.266.2.L113.

Abstract

We investigated the distribution of endothelin A (ETA) and ETB receptors in single smooth muscle cells and their contribution to ET-induced contractions of guinea pig trachea. ETA and ETB receptors were detected in smooth muscle membranes (maximum binding capacities of 810 and 360 fmol/mg protein and dissociation constants of 38 and 5.1 pM for 125I-labeled ET-1 and 125I-ET-3, respectively) and visualized autoradiographically in primary cultured cells. ET-1 and ET-3 evoked concentration-dependent increases in intracellular Ca2+ concentration and smooth muscle tension. The half-maximally effective concentrations of ET-1 and ET-3 at inducing contractions were 1.9 and 2.7 nM, respectively. The Ca2+ responses showed tachyphylaxis to both ETs after stimulation with ET-1, but only to ET-3 after stimulation with ET-3. Consecutive applications of ET-3 and ET-1 (10 nM each) classified the cells into ETA dominant (approximately 30%) responding to only ET-1, ETB dominant (approximately 20%) responding to only ET-3, and ETA- and ETB-possessing (approximately 50%) cells responding to both. The ETA antagonist, 10 microM BQ-123, attenuated ET-1-induced contractions but did not affect the ET-3-induced contractions. The results indicate that both receptors coexist in a major population of smooth muscle cells and cooperate in mediating ET-1-induced contractions.

MeSH terms

  • Animals
  • Binding Sites
  • Calcium / metabolism
  • Cells, Cultured
  • Endothelins / pharmacology
  • Fura-2
  • Guinea Pigs
  • Intracellular Membranes / metabolism
  • Male
  • Muscle Contraction / physiology*
  • Muscle, Smooth / cytology
  • Muscle, Smooth / metabolism*
  • Muscle, Smooth / physiology*
  • Osmolar Concentration
  • Receptors, Endothelin / metabolism*
  • Trachea / cytology
  • Trachea / metabolism*
  • Trachea / physiology*

Substances

  • Endothelins
  • Receptors, Endothelin
  • Calcium
  • Fura-2