Quaternary ammonium salt derivative of haloperidol inhibits KCl-induced calcium increase in rat aortic smooth muscle cells
Abstract
Aim: To study the effect of quaternary ammonium salt derivative of haloperidol (F3) on intracellular calcium (Ca2+) dynamic change in vascular smooth muscle cells (VSMC).
Methods: Using laser confocal scanning microscopy (LCSM), to observe the effect of F3 (0.01 - 10 micromol/L) on increase of intracellular Ca2+ fluorescent intensity induced by KCl (30 mmol/L) in VSMC.
Results: KCl induced a rapid increase of intracellular Ca2+ fluorescent intensity. F3 inhibited the rapid increase of that in both concentration-dependent manner (KCl: 67 +/- 24; F3 0.01 micromol/L: 57 +/- 13; 0.1 micromol/L: 40 +/- 13; 1 micromol/L: 29 +/- 9; 10 micromol/L: 20 +/- 6) and time-dependent manner; during 0 - 30 s after F3 was added, the change of fluorescent intensity was more rapid.
Conclusion: The inhibitory effect of F3 on Ca2+ concentration in VSMC was mainly due to the blocking of the Ca2+ influx, and might partially attributed to opening of the potassium (K+) channel.
Keywords:
Methods: Using laser confocal scanning microscopy (LCSM), to observe the effect of F3 (0.01 - 10 micromol/L) on increase of intracellular Ca2+ fluorescent intensity induced by KCl (30 mmol/L) in VSMC.
Results: KCl induced a rapid increase of intracellular Ca2+ fluorescent intensity. F3 inhibited the rapid increase of that in both concentration-dependent manner (KCl: 67 +/- 24; F3 0.01 micromol/L: 57 +/- 13; 0.1 micromol/L: 40 +/- 13; 1 micromol/L: 29 +/- 9; 10 micromol/L: 20 +/- 6) and time-dependent manner; during 0 - 30 s after F3 was added, the change of fluorescent intensity was more rapid.
Conclusion: The inhibitory effect of F3 on Ca2+ concentration in VSMC was mainly due to the blocking of the Ca2+ influx, and might partially attributed to opening of the potassium (K+) channel.