Display Settings:

Format

Send to:

Choose Destination

    J Biomed Sci. 2007 Jan;14(1):129-43. Epub 2007 Feb 3.

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

    Chung WS, Farley JM.

    Department of Pharmacology and Toxicology, University of Mississippi Medical Center, Jackson, MS 39216-4505, USA.

    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.

    PMID: 17278012 [PubMed - indexed for MEDLINE]

    Supplemental Content

    Patient drug information

    • Verapamil (Calan®, Calan® SR, Covera-HS®, ...)

      Verapamil is used to treat high blood pressure and to control angina (chest pain). The immediate-release tablets are also used alone or with other medications to prevent and treat irregular heartbeats. Verapamil is in a ...

    • Nifedipine (Adalat®, Adalat® CC, Afeditab® CR, ...)

      Nifedipine is used to treat high blood pressure and to control angina (chest pain). Nifedipine is in a class of medications called calcium-channel blockers. It works by relaxing the blood vessels so the heart does not ha...

    • Nicardipine (Cardene®, Cardene® SR)

      Nicardipine is used to treat high blood pressure. It relaxes your blood vessels so your heart does not have to pump as hard. It also increases the supply of blood and oxygen to the heart to control chest pain (angina). I...