1-(2,6-二甲基苯氧基)-2-(3,4-二甲氧基苯乙胺基)丙烷盐酸盐对实验性高血压大鼠的降压作用

DDPH 3～10 mg/kg iv降低DOCA—盐型及自发性高血压(SH)大鼠的MAP及HR;50,100mg/kg ig降低清醒正常血压及SH大鼠MAP及HR·心率减慢较降压作用持续时间短。DDPH(10,100μmol/L)对犬乳头状肌收缩力及静息30 s后第一次收缩(PRC_(30))有抑制作用。小鼠ig DDPH的LD_(50)为640 mg/kg,95％可信限为567～713mg/kg。麻醉大鼠静脉恒速灌注DDPH的致死量为47±SD 4 mg/kg。表明DDPH对实验性高血压大鼠有降压作用,并对心肌收缩力及肌浆网Ca~(2+)的释放有轻度抑制作用。

Hypotensive effects of 1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino) propane hydrochloride on experimental hypertensive rats

1-(2,6-dimethylphenoxy)-2-(3,4-dimethoxyphenylethylamino)propane hydrochloride(DDPH),a new synthetic compound,3-10 mg/kg iv dose-dependently decreased mean arterial pressure(MAP)in the anaesthetized DOCA-salt hypertensive rats and conscious spontaneously hypertensive rats(SHR).DDPH reduced heart rate(HR)simultaneously; however,HR recovered to its initial value more quickly than MAP.DDPH 50-100 mg/kg given orally also decreased MAP and HR in the conscious normotensive rats and conscious SHR.DDPH(0.1-1μmol/L)had no significant influence on contractility and the postrest contraction after resting 30 seconds(PRC30)in canine papillary muscles.DDPH(10-100μmol/L)significantly inhibited theforce of contraction and PRC30 in canine papillary muscles.The LD50 value of DDPH(ig)is 640 mg/kg in mice.The lethal dose of DDPH(iv infusion)is 47±SD 4 mg/kg in the pentobarbitone-anaesthe-tized rats.The results demonstrated that DDPH has an antihypertensive effects on the experimental hypertensive rats.DDPH has a slight inhibitory effect on the contractility and calcium release from sarcoplasmic reticulum in canine papillary muscles.