Ida H
Arzneimittelforschung. 1976;26(7):1337-40.
The beta-stimulant activity of 3-formylamino-4-hydroxy-alpha-(N-1-methoxyphenethylaminomethyl)-benzylalcohol-hemifumarate (BD 40A) was compared with those of isoproterenol, orciprenaline, trimetoquinol and salbutamol in conscious guinea pigs. Bronchodilator effects of BD 40A were most potent among five agonists by s.c., oral and aerosol administration, and were lasting by oral and aerosol administration. BD 40A was similar to isoproterenol, more potent than trimetoquinol, orciprenaline and salbutamol in increasing heart rate by s.c. route. The cardiostimulating effect of BD 40A was more potent than that of isoproterenol, trimetoquinol and salbutamol orally. However, the order of bronchoselectivity (ratio between ED30 beats/min vs. ED50) in conscious guinea pigs was salbutamol greater than BD 40A = trimetoquinol greater than orciprenaline greater than isoproterenol by s.c. administration, and by oral administration the order was BD 40A = salbutamol greater than trimetoquinol = isoproterenol. Orciprenaline showed no beta-stimulating effect in guinea pigs orally. In guinea pigs, BD 40A, like salbutamol, seems to be a beta2-adrenoceptor stimulant.
在清醒豚鼠中，比较了3-甲酰氨基-4-羟基-α-(N-1-甲氧基苯乙胺甲基)-苄醇半富马酸盐（BD 40A）与异丙肾上腺素、奥西那林、曲美托喹酚和沙丁胺醇的β-激动剂活性。通过皮下、口服和气雾剂给药，BD 40A的支气管扩张作用在五种激动剂中最为显著，且口服和气雾剂给药后作用持久。BD 40A通过皮下途径增加心率的作用与异丙肾上腺素相似，比曲美托喹酚、奥西那林和沙丁胺醇更强。口服时，BD 40A的心脏刺激作用比异丙肾上腺素、曲美托喹酚和沙丁胺醇更强。然而，在清醒豚鼠中，皮下给药时支气管选择性（ED30次/分钟与ED50的比值）的顺序为沙丁胺醇＞BD 40A = 曲美托喹酚＞奥西那林＞异丙肾上腺素，口服给药时顺序为BD 40A = 沙丁胺醇＞曲美托喹酚 = 异丙肾上腺素。奥西那林口服时在豚鼠中未显示出β-刺激作用。在豚鼠中，BD 40A与沙丁胺醇一样，似乎是一种β2-肾上腺素能受体激动剂。
