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The Difference Between Nicardipine and Its Enantiomers on Inhibiting Vasoconstriction of Isolated Rabbit Thoracic Artery

Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea, v.28 no.3, 2005년, pp.319 - 324  

Wang Sicen (College of Pharmacy, Xi'an Jiaotong University) ,  He Lang chong (College of Pharmacy, Xi'an Jiaotong University) ,  Yun Sofeng (College of Pharmacy, Xi'an Jiaotong University)

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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 wer...

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제안 방법

  • In this paper, the two enantiomers of nicardipine were prepared by using a high performance liq니id chromatographic system equipped with a Chiralcel OJ column. The inhibitions of vasoconstriction for nicardipine and its enentiomers were investigated by arterial strip trial in vitro, respectively.
  • The maximum responses to these three agents were set as 100%, respectively. Then the three different concentrations (0.1 mm이・L너, 0.5 mmol-L'1, and 1.0 mmol-L'1of each drug [(+)- NCD, S-(+)-NCD and F?-(-)-NCD] were tested on the three kind of models, respectively. The results indicated that (土)-NCD, S-(+)-NCD and ff-(-)-NCD could shift the doseresponse curves to right in a nonparallel manner (Fig.

대상 데이터

  • The binodrenal injection solution (NE, 2 mg, 10x 1 mL) was obtained from Wuhan Pharmaceutical Plant (W나lan, China). Potasshjm chloride (KCI) and calci니m chloride (CaCI2) were obtained from Xi'an Chemical Reagent Plant (Xi'an, China). All the other chemicals were of analytical reagent grade unless otherwise indicated.
  • Rabbits (male or female, 2.0-2.5 kg) were supplied by the Experimental Animal Center of Xi'an Jiaotong University (Xi'an, China).

이론/모형

  • The hexane in solution was evaporated under conditions of darkness and a nitrogen gas stream, and the ethanol solution containing each enantiomer was so obtained. The purities of enantiomers were analyzed by using the chiral HPLC method described above.
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참고문헌 (14)

  1. 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) 

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

  3. 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) 

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

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

  6. 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) 

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

  8. Kanamori, 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) 

  9. 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) 

  10. Takenaka, T., Miyazuki I, Asano M, et al., Vasodilator and hypotensive effects of the optical isomers of nicardipine(YC- 93), a new $Ca^{2+}$ -antagonist. Jpn. J. Pharmacol., 32, 665-670 (1982) 

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

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

  13. 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) 

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

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