Ragone María Inés, Bayley Matías, López Sofía, Díaz Romina G, Consolini Alicia E
Cátedra de Farmacología, Grupo de Farmacología Experimental y Energética Cardíaca (GFEYEC), Departamento de Ciencias Biológicas, Facultad de Ciencias Exactas, Universidad Nacional de La Plata (UNLP), 47 y 115 (1900) La Plata, La Plata, Argentina.
Centro de Investigaciones Cardiovasculares (CIC-UNLP-CONICET), La Plata, Argentina.
Naunyn Schmiedebergs Arch Pharmacol. 2024 May;397(5):3093-3109. doi: 10.1007/s00210-023-02791-0. Epub 2023 Oct 25.
Nebivolol could prevent dysfunction in patients suffering myocardial ischemia. However, influence of hyperthyroidism is not known. Consequences and mechanisms of nebivolol treatment were investigated in isolated hearts from euthyroid (EuT) and hyperthyroid (HpT) rats. Rats were orally treated during 1 week with 20 mg/kg/day nebivolol (O-Neb), 30 mg/kg/day atenolol (O-Ate), or not treated (C). Isolated perfused hearts were exposed to global ischemia and reperfusion (I/R) inside a flow calorimeter. Left diastolic ventricular pressure, developed contractile pressure (P), and total heat rate (Ht) were continuously measured, while infarct size was measured after 2-h R. EuT-C and HpT-C hearts developed similarly low post-ischemic contractile recovery and economy (P/Ht). Nebivolol totally prevented dysfunction and reduced infarction size in EuT hearts, but partially improved recovery in HpT rat hearts. Contrarily, oral atenolol totally prevented dysfunction in HpT hearts but partially in EuT hearts. Nebivolol effects were reversed by perfusing L-NAME in both conditions, but partially reduced by aminoguanidine in HpT. However, L-NAME increased P and P/Ht recoveries in EuT-C and HpT-C rat hearts, as well as melatonin. Oral nebivolol prevented post-ischemic dysfunction and infarction in EuT hearts due to adrenergic β1 blockade and activation of iNOS and/or eNOS, but the effect was attenuated in HpT hearts by excessive iNOS-dependent nitrosative pathways.
奈必洛尔可预防心肌缺血患者的功能障碍。然而,其对甲状腺功能亢进的影响尚不清楚。本研究在正常甲状腺(EuT)和甲状腺功能亢进(HpT)大鼠的离体心脏中,研究了奈必洛尔治疗的后果和机制。大鼠连续1周口服20mg/kg/天的奈必洛尔(O-Neb)、30mg/kg/天的阿替洛尔(O-Ate)或不进行治疗(C)。将离体灌注心脏置于血流热量计中进行全心缺血再灌注(I/R)。连续测量左心室舒张压、收缩压(P)和总热率(Ht),再灌注2小时后测量梗死面积。EuT-C和HpT-C心脏缺血后收缩恢复和经济性(P/Ht)同样较低。奈必洛尔完全预防了EuT心脏的功能障碍并减小了梗死面积,但仅部分改善了HpT大鼠心脏的恢复情况。相反,口服阿替洛尔完全预防了HpT心脏的功能障碍,但仅部分预防了EuT心脏的功能障碍。在两种情况下,灌注L-NAME均可逆转奈必洛尔的作用,但在HpT中,氨基胍可部分降低其作用。然而,L-NAME以及褪黑素均可提高EuT-C和HpT-C大鼠心脏的P和P/Ht恢复率。口服奈必洛尔可通过阻断肾上腺素能β1以及激活诱导型一氧化氮合酶(iNOS)和/或内皮型一氧化氮合酶(eNOS)来预防EuT心脏缺血后的功能障碍和梗死,但在HpT心脏中,由于过度的iNOS依赖性亚硝化途径,其作用减弱。