The difference between nicardipine and its enantiomers on inhibiting vasoconstriction of isolated rabbit thoracic artery
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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 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.
Key wordsNicardipine Enantiomers Vasoconstriction Stereoselectivity
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