Thromboxane A2 receptor linked with the Ca2+ pathway in rat colonic crypt cells

Biochem Biophys Res Commun. 1999 May 19;258(3):708-12. doi: 10.1006/bbrc.1999.0674.

Abstract

To clarify the presence of thromboxane A2 (TXA2) receptor in the colonic epithelium, we examined the effect of 9,11-epithio-11, 12-methano-thromboxane A2 (STA2), a stable analogue of TXA2, on intracellular free Ca2+ concentration ([Ca2+]i) of indo-1-loaded single cells in isolated rat colonic crypts by laser confocal microscopy. STA2 increased [Ca2+]i in a concentration-dependent manner with a transient peak phase and a subsequent plateau phase. The EC50 values at peak and plateau phases were 1 and 32 nM, respectively. The STA2-induced increase in [Ca2+]i was completely blocked by two selective TXA2 receptor antagonists, KW-3635 and ONO-3708. These antagonists did not affect both the basal [Ca2+]i and the carbaco-induced increase in [Ca2+]i. Prostaglandin E2 did not increase [Ca2+]i. These results indicate that the STA2-elicited increase in [Ca2+]i is mediated specifically by a TXA2 receptor in colonic crypt cells This is the first report showing the presence of a TXA2 receptor that is associated with Ca2+ mobilization in the colon.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Benzimidazoles / pharmacology
  • Benzoxepins / pharmacology
  • Calcium / metabolism*
  • Colon / cytology
  • Colon / drug effects*
  • Colon / metabolism
  • Female
  • In Vitro Techniques
  • Rats
  • Rats, Wistar
  • Receptors, Thromboxane / agonists
  • Receptors, Thromboxane / metabolism*
  • Thromboxane A2 / analogs & derivatives
  • Thromboxane A2 / pharmacology

Substances

  • Benzimidazoles
  • Benzoxepins
  • Receptors, Thromboxane
  • Thromboxane A2
  • STA 2
  • ONO 3708
  • Calcium
  • KW 3635