Drexler H, Wollschläger H, Löllgen H, Just H
Arzneimittelforschung. 1981;31(1a):259-62.
Invasive cardiac measurements were performed at rest and during exercise after i.v. infection of 0.7 mg/kg 2-[(2-methoxy-4-methylsulfinyl)phenyl]-1H-imidazo[4,5-b]pyridine (AR-L 115 BS) in 10 patients with heart failure in NYHA class II and III of various origins. At rest AR-L 115 BS increased the cardiac index by 0.74 l/min/m2 (p less than 0.01) and the heart rate by 10 beats/min (p less than 0.01). Mean arterial pressure and pressures in the pulmonary artery and in the pulmonary capillary bed were not changed significantly. Stroke work index remained unchanged. At the highest comparable workload AR-L 115 BS reduced the pulmonary capillary wedge pressure by 7 mm Hg (p less than 0.001) and the mean pulmonary arterial pressure by 8 mm Hg (p less than 0.001). The other parameters measured did not change significantly. In most of the patients there was a reduction in the pulmonary capillary pressure in parallel with a slight increase in the stroke work index, indicating an improvement in left ventricular pump function. Four patients reported bright vision immediately after injection which lasted for several hours in 1 patient and for about 5 min in the others. One patient developed muscle tremor which lasted for several hours. The results suggest that AR-L 115 BS exerts a vasodilating action on the capacitance vessels and a positive-inotropic effect on the heart.
对10例不同病因的纽约心脏协会(NYHA)II级和III级心力衰竭患者静脉注射0.7mg/kg的2-[(2-甲氧基-4-甲亚磺酰基)苯基]-1H-咪唑并[4,5-b]吡啶(AR-L 115 BS)后,在静息和运动状态下进行有创心脏测量。静息时,AR-L 115 BS使心脏指数增加0.74 l/min/m²(p<0.01),心率增加10次/分钟(p<0.01)。平均动脉压、肺动脉压和肺毛细血管压无明显变化。每搏功指数保持不变。在最高可比工作量时,AR-L 115 BS使肺毛细血管楔压降低7mmHg(p<0.001),平均肺动脉压降低8mmHg(p<0.001)。所测量的其他参数无明显变化。大多数患者肺毛细血管压降低,同时每搏功指数略有增加,表明左心室泵功能改善。4例患者注射后立即出现视物明亮,1例持续数小时,其他患者持续约5分钟。1例患者出现肌肉震颤,持续数小时。结果表明,AR-L 115 BS对容量血管有血管舒张作用,对心脏有正性肌力作用。