Cardioprotective and β-adrenoceptor antagonistic activity of a newly synthesized aryloxypropanolamine derivative PP-36
Lokesh K Bhatt,1 Jyotika Bansal,2 Poonam Piplani,2 SL Bodhankar,3 A Veeranjaneyulu1
1Department of Pharmacology, School of Pharmacy and Technology Management, NMIMS University, Mumbai, India; 2University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India; 3Department of Pharmacology, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandawane, Pune, India
Abstract: The present study was performed to evaluate the cardioprotective effects and pharmacological characterization of newly synthesized β-adrenoreceptor antagonists 3-(3-tertbutylamino- 2-hydroxypropoxy)-4-methoxybenzaldehyde (PP-36) in the rat model of coronary artery occlusion and reperfusion. Pre-ischemic administration (20 minutes before coronary occlusion) of PP-36 showed cardioprotective effects against ischemia/reperfusion injury in rats. PP-36 (6 mg kg-1) significantly reduced arrhythmia score (6.33 ± 0.55, P < 0.05), infarct size/left ventricle size (38.9 ± 3.2, P < 0.05) and no mortality compared to vehicle-treated control group (14.17 ± 1.83, 44.9 ± 4.6 and 17% respectively). In-vitro studies in rat isolated right atria, guinea-pig trachea and rat distal colon preparations, were carried out to investigate the potency of PP-36 towards different β-adrenoceptor subtypes. pA2/pKB values of PP-36 for β1- β2- and β3-adrenoceptors were 6.904 ± 0.190, 6.44 ± 0.129 and 5.773 ± 0.129, respectively. In conclusion, PP-36 is a β-adrenoceptor antagonist possessing potent anti-arrhythmic and cardioprotective effects against ischemia/reperfusion injury in rats.
Keywords: β-adrenoreceptors blocker, ischemia/reperfusion injury, arrhythmias, infarct area
This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms.php and incorporate the Creative Commons Attribution - Non Commercial (unported, v3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.Download Article [PDF]