Tachyphylaxis to the inhibitory effect of L-type channel blockers on ACh-induced [Ca2+]i oscillations in porcine tracheal myocytes

J Biomed Sci. 2007 Jan;14(1):129-43. doi: 10.1007/s11373-006-9122-6. Epub 2007 Feb 3.

Abstract

Discrepancies about the role of L-type voltage-gated calcium channels (VGCC) in acetylcholine (ACh)-induced [Ca(2+)](i) oscillations in tracheal smooth muscle cells (TSMCs) have been seen in recent reports. We demonstrate here that ACh-induced [Ca(2+)](i) oscillations in TMCS were reversibly inhibited by three VGCC blockers, nicardipine, nifedipine and verapamil. Prolonged (several minutes) application of VGCC blockers, led to tachyphylaxis; that is, [Ca(2+)](i) oscillations resumed, but at a lower frequency. Brief (15-30 s) removal of VGCC blockers re-sensitized [Ca(2+)](i) oscillations to inhibition by the agents. Calcium oscillations tolerant to VGCC blockers were abolished by KB-R7943, an inhibitor of the reverse mode of Na(+)/Ca(2+) exchanger (NCX). KB-R7943 alone also abolished ACh-induced [Ca(2+)](i) oscillations. Enhancement of the reverse mode of NCX via removing extracellular Na(+) reversed inhibition of ACh-induced [Ca(2+)](i) oscillations by VGCC blockers. Inhibition of non-selective cation channels using Gd(3+) slightly reduced the frequency of ACh-induced [Ca(2+)](i) oscillations, but did not prevent the occurrence of tachyphylaxis. Altogether, these results suggest that VGCC and the reverse mode of NCX are two primary Ca(2+) entry pathways for maintaining ACh-induced [Ca(2+)](i) oscillations in TSMCs. The two pathways complement each other, and may account for tachyphylaxis of ACh-induced [Ca(2+)](i) oscillations to VGCC blockers.

MeSH terms

  • Animals
  • Calcium / metabolism*
  • Calcium Channel Blockers / pharmacology*
  • Calcium Channels, L-Type / metabolism*
  • Calcium Signaling / drug effects*
  • Cells, Cultured
  • Myocytes, Smooth Muscle / metabolism*
  • Swine
  • Trachea / cytology
  • Trachea / metabolism*

Substances

  • Calcium Channel Blockers
  • Calcium Channels, L-Type
  • Calcium