Quaternary ammonium salt derivative of haloperidol inhibits KCl-induced calcium increase in rat aortic smooth muscle cells.
OBJECTIVE
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.


CONCLUSIONS
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.
Shi
G G
GG
Department of Pharmacology, Shantou University Medical College, Shantou 515031, China ggshi@stu.edu.cn
Fang
H
H
Zheng
J H
JH
D000473:Alkanes / Q000494:pharmacology*; D000818:Animals; D001013:Aorta, Thoracic / Q000166:cytology / Q000378:metabolism; D001693:Biological Transport, Active / Q000187:drug effects; D002118:Calcium / Q000378:metabolism*; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D002478:Cells, Cultured; D006220:Haloperidol / Q000031:analogs & derivatives; D018613:Microscopy, Confocal; D009131:Muscle, Smooth, Vascular / Q000166:cytology / Q000378:metabolism*; D011189:Potassium Chloride / Q000494:pharmacology; D000644:Quaternary Ammonium Compounds / Q000494:pharmacology*; D051381:Rats; D017207:Rats, Sprague-Dawley
D000473:Alkanes; D002121:Calcium Channel Blockers; D000644:Quaternary Ammonium Compounds; C413608:quaternary bisammonium salt; D011189:Potassium Chloride; D006220:Haloperidol; D002118:Calcium