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Adv Pharm Bull. 2011;1(1): 10-17.
doi: 10.5681/apb.2011.002
PMID: 24312751
PMCID: PMC3849999
Scopus ID: 84875912385
  Abstract View: 1156
  PDF Download: 795

Original Research

Vasorelaxant Effect of a Newly Synthesized Dihydropyridine Ethyl Ester (DHPEE) on Rat Thoracic Aorta: Dual Mechanism of Action

Hossein Babaei*, Farzaneh Ebrahimi, Javid Shahbazi Mojarrad, Yadollah Azarmi, Afsaneh Gharehbagheri
*Corresponding Author: Email: babaeih@tbzmed.ac.ir

Abstract

Introduction: DHPEE is a newly synthesized compound by merging the key structural elements in an angiotensin receptor blocker (Telmisartan) with key structural elements in 1,4- dihydropyridine calcium channel blocker (Nifedipine). In this study, we examined dual calcium channel blocking and AT1 antagonist activity for DHPEE. Methods: The functional inhibitory characteristics of DHPEE were studied in vitro in rat thoracic aorta preparations precontracted by phenylephrine (1µM) or KCl (80µM) or Ang II in normal or calcium-free solutions. Results:Concentration–dependent significant relaxation was observed in aortic rings precontracted with phenylephrine, KCl or Ang II. The tension increment produced by increasing external calcium was also reduced by DHPEE. DHPEE caused a marked decrease in the maximal contractile response of the vasoactive agents and shifted their concentration-response curves to the right. Conclusion:DHPEE possesses dual characteristics and cause vasorelaxation by blocking the L-type calcium channels and blocking Ang II receptors (AT1) in rat aortic smooth muscle.
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Submitted: 08 May 2011
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