Pérez-Ojeda E, Hernandez J, Serrano J S
J Pharmacol. 1983 Jul-Sep;14(3):303-9.
The protective effect of phenytoin against an electroshock lethal dose (ELD), was compared with that of three different beta-blocking agents. These compounds were propranolol with quinidine-like activity (QLA) but no intrinsic sympathomimetic activity (ISA), practolol with ISA but no QLA and metoprolol with no ISA but some QLA. Phenytoin (15 mg/kg) and propranolol (70 mg/kg) protected all the animals. Metoprolol was only effective at higher concentrations (130 mg/kg). Practolol afforded some degree of protection at low doses (20 mg/kg) but at higher doses its ISA can be deleterious by decreasing the ELD threshold. These results suggest that QLA is more important than beta-blocking activity for protection against electroshock lethality.
将苯妥英对电休克致死剂量(ELD)的保护作用与三种不同的β受体阻滞剂进行了比较。这些化合物分别是具有奎尼丁样活性(QLA)但无内在拟交感活性(ISA)的普萘洛尔、具有ISA但无QLA的心得宁以及无ISA但有一定QLA的美托洛尔。苯妥英(15毫克/千克)和普萘洛尔(70毫克/千克)保护了所有动物。美托洛尔仅在较高浓度(130毫克/千克)时有效。心得宁在低剂量(20毫克/千克)时提供了一定程度的保护,但在高剂量时,其ISA可能会通过降低ELD阈值而产生有害作用。这些结果表明,对于预防电休克致死性,QLA比β受体阻滞活性更重要。