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一种新合成的芳氧基丙醇胺衍生物PP-36的心脏保护和β-肾上腺素能受体拮抗活性

Cardioprotective and β-adrenoceptor antagonistic activity of a newly synthesized aryloxypropanolamine derivative PP-36.

作者信息

Bhatt Lokesh K, Bansal Jyotika, Piplani Poonam, Bodhankar S L, Veeranjaneyulu A

机构信息

Department of Pharmacology, School of Pharmacy and Technology Management, NMIMS University, Mumbai, India.

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

J Exp Pharmacol. 2010 Feb 11;2:37-45. doi: 10.2147/jep.s8960. eCollection 2010.

DOI:10.2147/jep.s8960
PMID:27186089
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC4863284/
Abstract

The present study was performed to evaluate the cardioprotective effects and pharmacological characterization of newly synthesized β-adrenoreceptor antagonists 3-(3-tert-butylamino-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.

摘要

本研究旨在评估新合成的β-肾上腺素能受体拮抗剂3-(3-叔丁基氨基-2-羟基丙氧基)-4-甲氧基苯甲醛(PP-36)在大鼠冠状动脉闭塞和再灌注模型中的心脏保护作用及药理学特性。PP-36在缺血前给药(冠状动脉闭塞前20分钟)对大鼠缺血/再灌注损伤显示出心脏保护作用。与溶剂处理的对照组相比(分别为14.17±1.83、44.9±4.6和17%)，PP-36(6mg/kg)显著降低心律失常评分(6.33±0.55，P<0.05)、梗死面积/左心室面积(38.9±3.2，P<0.05)且无死亡情况。在大鼠离体右心房、豚鼠气管和大鼠远端结肠制剂中进行了体外研究，以研究PP-36对不同β-肾上腺素能受体亚型的作用强度。PP-36对β1-、β2-和β3-肾上腺素能受体的pA2/pKB值分别为6.904±0.190、6.44±0.129和5.773±0.129。总之，PP-36是一种β-肾上腺素能受体拮抗剂，对大鼠缺血/再灌注损伤具有有效的抗心律失常和心脏保护作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f61/4863284/8a8f411e2325/jep-2-037Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f61/4863284/f99a4aab99a2/jep-2-037Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f61/4863284/e65512875be8/jep-2-037Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f61/4863284/8a8f411e2325/jep-2-037Fig3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f61/4863284/f99a4aab99a2/jep-2-037Fig1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f61/4863284/e65512875be8/jep-2-037Fig2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2f61/4863284/8a8f411e2325/jep-2-037Fig3.jpg

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