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Journal of Pharmacology and Toxicology
  Year: 2006 | Volume: 1 | Issue: 2 | Page No.: 126-133
DOI: 10.3923/jpt.2006.126.133
 
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Synthesis and Biological Evaluation of 1-(2’, 4’-dimethoxyphenacyl)-4-acetyl-4-phenylpiperidinium bromide in Intestinal and Cardiovascular Tissues

Syed I.H. Taqvi, Mohammad T. Aftab, Muhammad N. Ghayur, Anwar H. Gilani and Zafar S. Saify

Abstract:
1-(2’, 4’-dimethoxyphenacyl)- 4-acetyl-4-phenylpiperidinium bromide is a synthetic piperidine compound which was screened in isolated intestinal and aortic smooth muscle and Langendorff’s heart preparations. The test compound exhibited dose-dependent spasmolytic effect on the spontaneous and high K+ (75 mM) contracted isolated rabbit jejunum with respective EC50 values of 0.08 mM (0.05-0.13, 95% CI) and 0.12 mM (0.06-0.21). The Ca++ channel blocking (CCB) activity was confirmed when the test compound (0.05-0.1 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 high K+ (75 mM)-induced contractions with an EC50 value of 0.04 mM (0.02-0.08) while also suppressed the norepinephrine (1 μM) peak responses with an EC50 value of 0.04 mM (0.03-0.06). When tested in Langendorff perfused rabbit heart preparation, it exhibited a negative inotropic effect in the ventricles with EC50 value of 0.59 mM (0.04-8.86) with negligible effect on the rate of ventricular contractions. The results show inhibitory effects of the test compound on intestinal and vascular smooth muscle preparations and a cardio-suppressant effect, possibly mediated via blockade of voltage and receptor-operated Ca++ channels.
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How to cite this article:

Syed I.H. Taqvi, Mohammad T. Aftab, Muhammad N. Ghayur, Anwar H. Gilani and Zafar S. Saify, 2006. Synthesis and Biological Evaluation of 1-(2’, 4’-dimethoxyphenacyl)-4-acetyl-4-phenylpiperidinium bromide in Intestinal and Cardiovascular Tissues. Journal of Pharmacology and Toxicology, 1: 126-133.

DOI: 10.3923/jpt.2006.126.133

URL: https://scialert.net/abstract/?doi=jpt.2006.126.133

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