Literature DB >> 11749867

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

G G Shi1, H Fang, J H Zheng.   

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.

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Year:  2001        PMID: 11749867

Source DB:  PubMed          Journal:  Acta Pharmacol Sin        ISSN: 1671-4083            Impact factor:   6.150


  2 in total

1.  Design, synthesis, and pharmacological evaluation of haloperidol derivatives as novel potent calcium channel blockers with vasodilator activity.

Authors:  Yicun Chen; Jinhong Zheng; Fuchun Zheng; Jinzhi Wang; Yanmei Zhang; Fenfei Gao; Zhanqin Huang; Ganggang Shi
Journal:  PLoS One       Date:  2011-11-16       Impact factor: 3.240

2.  Characterization and bioactivity of novel calcium antagonists - N-methoxy-benzyl haloperidol quaternary ammonium salt.

Authors:  Yi-Cun Chen; Wei Zhu; Shu-Ping Zhong; Fu-Chun Zheng; Fen-Fei Gao; Yan-Mei Zhang; Han Xu; Yan-Shan Zheng; Gang-Gang Shi
Journal:  Oncotarget       Date:  2015-12-22
  2 in total

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