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Inhibition of Optical Isomers of p-Chlorobenzyltetrahydrober-berine on Vascular Smooth Muscle Contraction Caused by Ca ~(2+)

SUN Li 1,DAI De-Zai 2 1 Drug Screening Center,China Pharmaceutical University,Nanjing 210038;2 Department of Pharmacology,China Pharmaceutical University,Nanjing 210009,P.R.China  
AIM:To compare the effect of p-Chlorobenzyletrahydroberberine(CPU-86017)and its four kinds of optical isomers Zh001,Zh002,Zh003 and Zh004 on intracellular calcium mobilization and calcium entry by suppression on isolated vascular smooth contraction.METHODS:CPU-86017 and four kinds of optical isomers(10,30,100 μmol·L-1)were applied to suppress 6 kinds of contractions performed as below.Group 1:KCl(100 mmol·L-1)induced contractions in normal K-H solution;Group 2:KCl caused contractions in Ca 2+-free K-H solution;Group 3:contractions induced by adding 3.0 mmol·L-1 CaCl 2 to the Ca 2+-free K-H solution after using KCl caused contractions in Ca 2+-free K-H solution;Performing the same procedure as the former except for using phenylephrine instead of KCl.RESULTS:All the compounds inhibited the contraction induced by intracellular calcium release and extra-cellular calcium entry induced by KCl.The potencies of Zh003 and Zh004 were higher than that of CPU-86107 while Zh001 and Zh002 were lower.Zh004 had significant inhibitory effect on phenylephrine intracellular calcium release and extracellular calcium entry,and the effects of Zh001,Zh002 and Zh003 were faint.CONCLUSION:For the blocking effect on α-adrenergic receptor,Zh001,Zh002 and Zh003 decreased evidently when compared with CPU-86017.Zh003 almost had no blocking effect on receptor-operated channel.The inhibitory effects on voltage-depencled channel of Zh003 and Zh004 were increased.
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