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The difference between nicardipine and its enantiomers on inhibiting vasoconstriction of isolated rabbit thoracic artery

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Abstract

The present study was designed to study the difference effects between nicardipine and its two enantiomers on thoracic artery of rabbit. A high-performance liquid chromatographic method was used to prepare the two enantiomers of nicardipine. The thoracic artery of rabbit was removed. The vessels were cut into 3 mm in width and 15 mm in length spiral strips and immersed into tissue baths. The concentration-response curves of nicardipine and its enantiomers were obtained by cumulative administration of the vasoconstrictors. Nicardipine and the enantiomers could shift the dose-response curves of NE, KCI or CaCI2to right in a nonparallel manner and decrease the maximum effective in a concentration-depended manner, respectively. The pD2’ value of R-(-)-nicardipine showed significantly effective than that of nicardipine and S-(+)-nicardipine (P<0.01). There was not obviouse difference between the pD2’ value of nicardipine and S-(+)-nicardipine (R>0.05). The results demonstrate that the stereoselective interaction betweenR-(-)-nicardipine and L-calcium channel receptor is more stronger than that of S-(+)-nicardipine.

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References

  • Brisac, A. M., Champeroux, P., Lucet, B.,et al., Centrl peripheral effects of the optical isomers of nicardipine, a dihydropridines calcium channel antagonist, in rats.Eur. J. Pharmacol., 146, 171–174 (1988).

    Article  PubMed  CAS  Google Scholar 

  • Chen, Qi. In Method of TCM Pharmacological Experiment(First Edition), the Peoples Medical Publishing House, Beijing, 693–694 (1993).

    Google Scholar 

  • Fischer, C., Schonberger, F., Muck, W.,et al., Simultaneous assessment of the intravenous and oral disposition of the enantiomers of racemic nimodipine by chiral stationary phase high-performance liquid chromatography and gas chromatography/mass spectroscopy combined with a stable isotope technique.J. Pharm. Sci., 82, 244–250 (1993).

    Article  PubMed  CAS  Google Scholar 

  • Guan Li-xin, Yi Xin, Yang Liu-yanat al., Vasodilating mechanism of epimedium icariine.Chin. Pharm. Bull., 12, 320–321 (1996).

    Google Scholar 

  • H. Gerhard Vogel, and Wolfgang H. Vogel., Drug Discovery and Evaluation-Pharmacologicol Assays. Springer-Verlag Berlin Heidelberg, 135–136 (1997).

    Google Scholar 

  • Hoffman, R. P., and Vuorela, H. J., Assessing calcium antagonism on vascular smooth muscle: a comparison of the three method.J. Pharmacol. Methods, 9–41 (1983).

  • Jiang Guangzu. Study and development of chiral drug.Chin. Pharm. J., 31, 579–581 (1996).

    Google Scholar 

  • anamori, M., Naka, M., Asano, M.et al., Effective of N-(6-aminohexyl)-5-chloro-1-naphthalene-sulfonamide and other calmodulin antagonists (calmodulin interacting agents) on calcium induced contraction of rabbit aortic strips.J. Pharmacol. Exp. Ther., 217, 494–502 (1981).

    Google Scholar 

  • Terai, M., Takenaka, T., and Maeno, H., Inhibition of calcium influx in rabbit aorta by nicardipine hydrochloride (YC-93).Biochem. Pharmacol., 30, 375–378 (1981).

    Article  PubMed  CAS  Google Scholar 

  • Takenaka, T., Miyazuki I., Asano M.,et al., Vasodilator and hypotensive effects of the optical isomers of nicardipine(YC-93), a new Ca2+-antagonist.Jpn. J. Pharmacol., 32, 665–670 (1982).

    Article  PubMed  CAS  Google Scholar 

  • Tsukasa, U., Tadashi, O., and Kazunobu, S., Enantioselective high-liquid chromatographic determination of nicardipine in human plasma.J. Chromatogr. B., 698, 181–186 (1997).

    Article  Google Scholar 

  • Uno, T., Ohkubo, T., and Sugawara, K., Enantioselective high-performance liquid chromatographic determination of nicardipine in human plasma.J. Chromatogr. B, 698, 181–186 (1997).

    Article  CAS  Google Scholar 

  • Wang Sicen, Lui Fei, and He Langchong, Studies on differences of pharmacokinetic behavior and tissue distribution of nicardipine and its two enantiomers in rats by using achiral and chiral liquid chromatography.Acta Pharml. Sinica, 38, 603–608 (2003).

    Google Scholar 

  • Wolfgang, M. M., Enantiospecific determination of nimodipine in human plasma by liquid chromatography tandem mass spectrometry.J. Chromatogr. A, 712, 45–53 (1995).

    Article  Google Scholar 

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Authors and Affiliations

  1. College of Pharmacy, Xi’an-Jiaotong University, 710061, Xi’an, China

    Sicen Wang, Langchong He & Bofeng Yun

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  1. Sicen Wang
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  2. Langchong He
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  3. Bofeng Yun
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Correspondence to Langchong He.

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Wang, S., He, L. & Yun, B. The difference between nicardipine and its enantiomers on inhibiting vasoconstriction of isolated rabbit thoracic artery. Arch Pharm Res 28, 319–324 (2005). https://doi.org/10.1007/BF02977799

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  • DOI: https://doi.org/10.1007/BF02977799

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