Cardioprotective and β-adrenoceptor antagonistic activity of a newly synthesized aryloxypropanolamine derivative PP-36
| Autor: | Poonam Piplani, Addepalli Veeranjaneyulu, Lokesh Kumar Bhatt, Subhash L. Bodhankar, Jyotika Bansal |
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| Jazyk: | angličtina |
| Rok vydání: | 2010 |
| Předmět: |
medicine.medical_specialty
Coronary artery occlusion β-adrenoreceptors blocker infarct area Ischemia RM1-950 Pharmacology ischemia/reperfusion injury β adrenoceptor Internal medicine medicine Potency Pharmacology (medical) Original Research business.industry Antagonist medicine.disease medicine.anatomical_structure Journal of Experimental Pharmacology Coronary occlusion Ventricle Cardiology Molecular Medicine Therapeutics. Pharmacology business Reperfusion injury arrhythmias |
| Zdroj: | Journal of Experimental Pharmacology, Vol 2010, Iss default, Pp 37-45 (2010) Journal of Experimental Pharmacology |
| ISSN: | 1179-1454 |
| Popis: | Lokesh K Bhatt,1 Jyotika Bansal,2 Poonam Piplani,2 SL Bodhankar,3 A Veeranjaneyulu11Department 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, IndiaAbstract: 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 |
| Databáze: | OpenAIRE |
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