S.I. H. Taqvi
Federal Urdu University of Arts, Science and Technology, University Road, Karachi, Pakistan
M. N. Ghayur
Department of Biomedical and Biological Sciences, The Aga Khan University, Stadium Road, Karachi-74800, Pakistan
A. H. Gilani
Department of Biomedical and Biological Sciences, The Aga Khan University, Stadium Road, Karachi-74800, Pakistan
M. T. Aftab
Post Graduate Medical Institute, Baqai Medical University, Karachi, Pakistan
Z. S. Saify
Faculty of Pharmacy, University of Karachi, Karachi, Pakistan
ABSTRACT
The smooth muscle relaxant and cardiovascular suppressant activities of a newly synthesized piperidine derivative: (1-[4-methylphenacyl]-4-acetyl-4-phenylpiperidinium bromide) were studied in isolated tissue preparations. The test compound exhibited dose-dependent relaxant effect on the spontaneous and K+ (75 mM)-induced contractions of isolated rabbit jejunum with respective EC50 values of 0.056 mM (0.011-0.289, 95% CI) and 0.052 mM (0.004-0.769). The Ca++ channel blocking (CCB) activity was confirmed when the test compound (0.005-0.020 mM) shifted the Ca++ dose-response curves to the right, similar to that produced by verapamil (0.3-1.0 μM), a standard CCB. In the isolated rabbit aorta, the test compound showed a dose-dependent vasodilator effect on norepinephrine (1 μM) or K+ (75 mM)-induced contractions with an EC50 value of 0.016 mM (0.005-0.048). When tested in Langendorff perfused rabbit heart preparation, it exhibited a negative chronotropic effect in atria and ventricles with respective EC50 values of 0.79 mM (0.45-2.05) and 0.63 mM (0.32-1.52) and also a negative inotropic effect in atria and ventricles with respective EC50 values of 0.98 mM (0.30-3.19) and 8.98 mM (5.98-13.50). The results showed that inhibitory effects of the piperidine derivative on intestinal and cardiovascular preparations are mediated possibly via blockage of voltage and receptor-operated Ca++ channels.
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How to cite this article
S.I. H. Taqvi, M. N. Ghayur, A. H. Gilani, M. T. Aftab and Z. S. Saify, 2006. Synthesis, Spasmolytic, Cardio-suppressant, Vasodilator and Ca++ Antagonist Activities of 1-[4`-methylphenacyl]-4-acetyl -4-phenylpiperidinium bromide. Pakistan Journal of Biological Sciences, 9: 60-66.
DOI: 10.3923/pjbs.2006.60.66
URL: https://scialert.net/abstract/?doi=pjbs.2006.60.66
DOI: 10.3923/pjbs.2006.60.66
URL: https://scialert.net/abstract/?doi=pjbs.2006.60.66
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