• The Korean Journal of Physiology and Pharmacology
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• v.14 no.5
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• pp.305-310
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• 2010

The human $ether$-$a$-$go$-$go$-related gene ($hERG$) channel is important for repolarization in human myocardium and is a common target for drugs that prolong the QT interval. We studied the effects of two antipsychotics, tiapride and sulpiride, on hERG channels expressed in $Xenopus$ oocytes and also on delayed rectifier $K^+$ currents in guinea pig cardiomyocytes. Neither the amplitude of the hERG outward currents measured at the end of the voltage pulse, nor the amplitude of hERG tail currents, showed any concentration-dependent changes with either tiapride or sulpiride ($3{\sim}300{\mu}M$). However, our findings did show that tiapride increased the potential for half-maximal activation ($V_{1/2}$) of HERG at $10{\sim}300{\mu}M$, whereas sulpiride increased the maximum conductance ($G_{max}$) at 3, 10 and $100{\mu}M$. In guinea pig ventricular myocytes, bath applications of 100 and $500{\mu}M$ tiapride at $36^{\circ}C$ blocked rapidly activating delayed rectifier $K^+$ current ($I_{Kr}$) by 40.3% and 70.0%, respectively. Also, sulpiride at 100 and $500{\mu}M$ blocked $I_{Kr}$ by 38.9% and 76.5%, respectively. However, neither tiapride nor sulpiride significantly affected the slowly activating delayed rectifier $K^+$ current ($I_{Ks}$) at the same concentrations. Our findings suggest that the concentrations of the antipsychotics required to evoke a 50% inhibition of IKr are well above the reported therapeutic plasma concentrations of free and total compound.

• Archives of Pharmacal Research
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• v.27 no.9
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• pp.901-905
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• 2004

A rapid, sensitive and selective hydrophilic interaction liquid chromatography-tandem mass spectrometric(HILIC-MS/MS) method for the determination of tiapride in human plasma was developed. Tiapride and internal standard, metoclopramide were extracted from human plasma with dichloromethane at basic pH and analyzed on an Atlantis HILIC silica column with the mobile phase of acetonitrile-ammonium formate (190 mM, pH 3.0) (94：6, v/v). The ana-Iytes were detected using an electrospray ionization tandem mass spectrometry in the multi-ple-reaction-monitoring mode. The standard curve was linear (r＝0.999) over the concentration range of 1.00-200 ng/mL. The coefficient of variation and relative error for intra- and inter-assay at three QC levels were 6.4∼8.8％ and -2.0∼3.6％, respectively. The recoveries of tiapride ranged from 96.3 to 97.4％, with that of metoclopramide (internal standard) being 94.2％. The lower limit of quantification for tiapride was 1.00 ng/mL using 1 00 $\mu$L of plasma sample.

• Proceedings of the PSK Conference
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• 2002.10a
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• pp.400.3-401
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• 2002

Levosulpiride is the levo-enantiomer from of racemic sulpride. abenzamide derivative selectively inhibition doparninergic D2 receptos at the trigger zone both in the central nervous system and in the gastrointestinal tract. We report a rapid and sensitive HPLC method using reverse phase C 18 column with fluorescence detection for separation and quantitation of levosulpiride in plasma. Tiapride was used as an internal standard. After adding an internal standard. levosulpiride in 800 ${\mu}l$ of plasma was extracted under basic conditions with ethyl acetate and methylene chloride. (omitted)

• The Journal of Pediatrics of Korean Medicine
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• v.36 no.2
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• pp.13-25
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• 2022

Objective This study aimed to analyze randomized controlled trials of the effect of acupuncture on Tourette syndrome and to evaluate the efficacy of the treatment. Methods Based on the China National Knowledge Infrastructure (CNKI) and Pubmed search with the key search terms of 'Tourette syndrome, acupuncture', dated from 2000 to 2021, ten randomized controlled trials were identified and analyzed for this study. Results 1. The most commonly used acupoints were Taechung (LR3), Sinmun (HT7), Hapgok (LI4), Pungji (GB20) and Backhoe (GV20). 2. The most commonly used meridians were Bladder Meridian, Stomach Meridian and Gallbladder Meridian. 3. Acupuncture treatment was found to be significantly more or equally effective than western medicine such as haloperidol and tiapride. Conclusions Based on the results of the randomized controlled trials analyzed in this study, acupuncture was found to be effective in the treatment of Tourette syndrome. However, more clinical studies are needed to prove the effectiveness of acupuncture in Tourette syndrome.