Activity Induced by a Naphthalene-Prazosin Derivative on Ischemia/Reperfusion Injury in Rats  

作　　者：Betty Sarabia-Alcocer Lauro Figueroa-Valverde Francisco Díaz-Cedillo Lenin Hau-Heredia Marcela Rosas-Nexticapa Elodia García-Cervera Eduardo Pool-Gómez Rolando García-Martínez Braulio Zepeda-Acosta 

机构地区：[1]Laboratory of Pharmaco Chemistry, Faculty of Chemical and Biological Sciences, University Autonomous of Campeche, Campeche, México [2]Escuela Nacional de Ciencias Biológicas del Instituto Politécnico Nacional, México D.F., México [3]Facultad de Nutrición, Universidad Veracruzana, Veracruz, México [4]Laboratorio de Neurociencias del Centro de Investigaciones Biomédicas de la Universidad Autónoma de Campeche, Campeche, México

出　　处：《Pharmacology & Pharmacy》2014年第12期1130-1142,共13页药理与制药（英文）

摘　　要：In this study, a new naphthalene-prazosin derivative (compound 5) was synthetized with the objective of evaluating its activity on ischemia/reperfusion injury. The Langendorff technique was used to evaluate the effect of the compound 5 on ischemia/reperfusion injury. Additionally, the mechanism of action involved in the activity exerted by the compound 5 on perfusion pressure and coronary resistance was evaluated by measuring left ventricular pressure in absence or presence of following compounds;prazosin, metoprolol, indomethacin and nifedipine. The results showed that the compound 5 reduced infarct size compared with the control conditions. Other results showed that the compound 5 significantly increases (p = 0.05) the perfusion pressure and coronary resistance in isolated rat heart. In addition, other data indicate that the compound 5 increases left ventricular pressure in a dose-dependent manner (0.001 to 100 nM);however, this phenomenon was significantly inhibited by nifedipine at a dose of 1 nM (p = 0.05) and this effect was independent of cAMP levels. In conclusion, these data suggest that the naphthalene-prazosin derivative exerts a cardio protective effect via the calcium channels activation and consequently induces changes in the left ventricular pressure levels. This phenomenon results in a decrease of myocardial necrosis after ischemia and reperfusion.In this study, a new naphthalene-prazosin derivative (compound 5) was synthetized with the objective of evaluating its activity on ischemia/reperfusion injury. The Langendorff technique was used to evaluate the effect of the compound 5 on ischemia/reperfusion injury. Additionally, the mechanism of action involved in the activity exerted by the compound 5 on perfusion pressure and coronary resistance was evaluated by measuring left ventricular pressure in absence or presence of following compounds;prazosin, metoprolol, indomethacin and nifedipine. The results showed that the compound 5 reduced infarct size compared with the control conditions. Other results showed that the compound 5 significantly increases (p = 0.05) the perfusion pressure and coronary resistance in isolated rat heart. In addition, other data indicate that the compound 5 increases left ventricular pressure in a dose-dependent manner (0.001 to 100 nM);however, this phenomenon was significantly inhibited by nifedipine at a dose of 1 nM (p = 0.05) and this effect was independent of cAMP levels. In conclusion, these data suggest that the naphthalene-prazosin derivative exerts a cardio protective effect via the calcium channels activation and consequently induces changes in the left ventricular pressure levels. This phenomenon results in a decrease of myocardial necrosis after ischemia and reperfusion.

关 键 词：PRAZOSIN LEFT VENTRICULAR Pressure NIFEDIPINE NAPHTHALENE 

分 类 号：R73[医药卫生—肿瘤]