Srimal R C, Gulati K, Nityanand S, Dhawan B N
Central Drug Research Institute, Lucknow, India.
Pharmacol Res. 1990 May-Jun;22(3):319-29. doi: 10.1016/1043-6618(90)90729-w.
Hypotensive activity of 2-(2-(4-(3-methylphenyl)-1-piperazinyl)ethyl) quinoline (compound 71/73; centhaquin) was studied in cat and rat. The compound lowered the blood pressure and reduced the heart rate of anaesthetized and unanaesthetized (decerebrate) cat in a dose-dependent manner (0.01-1.0 mg/kg i.v. or 1.0-2.5 mg/kg intraduodenally). The hypotensive effect was insignificant in spinal transected cat but more marked in deafferented and vagotomized animals. Localization of centhaquin to brain by intravertebral arterial injection (5-10 micrograms) or by topical application to the exposed ventral surface of medulla or floor of the fourth ventricle caused hypotension and bradycardia as well as reduced the excitability of the vasomotor loci. It was also effective in rats after single as well as multiple dosing. The compound seems to act centrally to reduce the blood pressure.
研究了2-(2-(4-(3-甲基苯基)-1-哌嗪基)乙基)喹啉（化合物71/73；辛他喹）在猫和大鼠中的降压活性。该化合物以剂量依赖性方式降低麻醉和未麻醉（去大脑）猫的血压并降低心率（静脉注射0.01-1.0mg/kg或十二指肠内注射1.0-2.5mg/kg）。在脊髓横断的猫中降压作用不明显，但在去传入神经和迷走神经切断的动物中更显著。通过椎动脉内注射（5-10微克）或将其局部应用于暴露的延髓腹面或第四脑室底部，辛他喹在脑中的定位会引起低血压、心动过缓以及降低血管运动中枢的兴奋性。单次和多次给药后在大鼠中也有效。该化合物似乎通过中枢作用来降低血压。
