Yuki S, Hanazuka M, Watanabe T, Nishi H
Nihon Yakurigaku Zasshi. 1987 Apr;89(4):225-33. doi: 10.1254/fpj.89.225.
The hypotensive activity of terazosin has been attributed to inhibition of postsynaptic alpha-1 adrenoceptors. The present study examined the influence of terazosin on spontaneous sympathetic outflow in anesthetize and immobilized rats. The effects on blood pressure and heart rate were also evaluated. Intravenously (i.v.) injected terazosin 0.3 mg/kg and prazosin 0.1 mg/kg increased a sympathetic outflow by 15.4 and 21.6%, respectively. These drugs produced a significant and long-lasting fall in blood pressure with slight heart rate change. On the contrary, clonidine 0.1 mg/kg, i.v. significantly inhibited the sympathetic outflow by 69.2%. The intracerebroventricularly administered 10 micrograms/kg clonidine also showed the sympathoinhibitory effect. However 3 micrograms/kg, i.c.v. of terazosin and prazosin increased the sympathetic tone by 16 and 7.2%. During these periods, in both drugs slightly decreased the blood pressure. These changes in hemodynamic parameters and nerve activities were obtained at 2 approximately 3 min after the i.c.v. administration. The 10 micrograms/kg, i.c.v. of terazosin and prazosin significantly inhibited the pressor response by phenylephrine 1 micrograms/kg, i.v. These results indicate the peripheral effect of terazosin and prazosin through the penetration of the drugs from the brain. The results provide evidence that terazosin, like prazosin, dose not affect cardiovascular regulation by a central action.
特拉唑嗪的降压活性归因于对突触后α-1肾上腺素能受体的抑制。本研究检测了特拉唑嗪对麻醉并固定的大鼠自发交感神经传出的影响。还评估了其对血压和心率的作用。静脉注射0.3mg/kg特拉唑嗪和0.1mg/kg哌唑嗪分别使交感神经传出增加15.4%和21.6%。这些药物使血压显著且持久下降,心率变化轻微。相反,静脉注射0.1mg/kg可乐定可显著抑制交感神经传出69.2%。脑室内注射10μg/kg可乐定也显示出交感神经抑制作用。然而,脑室内注射3μg/kg特拉唑嗪和哌唑嗪可使交感神经张力分别增加16%和7.2%。在此期间,两种药物均使血压略有下降。这些血流动力学参数和神经活动的变化在脑室内给药后约2至3分钟获得。脑室内注射10μg/kg特拉唑嗪和哌唑嗪可显著抑制静脉注射1μg/kg去氧肾上腺素引起的升压反应。这些结果表明特拉唑嗪和哌唑嗪可通过药物从脑内渗透产生外周效应。结果提供了证据,表明特拉唑嗪与哌唑嗪一样,不会通过中枢作用影响心血管调节。