Rubin P C, Howden C W, McLean K, Reid J L
J Cardiovasc Pharmacol. 1982 Jul-Aug;4(4):527-30. doi: 10.1097/00005344-198207000-00001.
We conducted pharmacodynamic studies in man with a specific alpha 2-adrenoceptor agonist BHT-933. The study involved nine male normotensive volunteers each of whom received BHT-933 5 mg or placebo in random order. BHT-933 significantly lowered systolic and diastolic blood pressure (BP) in supine and standing positions, the greatest effect occurring 3-4 h following drug administration. Supine values: placebo 116/73; BHT-933 99/64. Standing values: placebo 114/79; BHT-933 92/67. Heart rate was uninfluenced by BHT-933 even at the time of maximum fall in BP. Plasma noradrenaline concentration in the supine position was significantly reduced: placebo 2.5 +/- 0.8 nmol/L; BHT-933 1.7 +/- 0.6. The haemodynamic changes accompanying Valsalva's manoeuvre and cold pressor test were uninfluenced by BHT-933. All subjects experienced sedation and dry mouth following BHT-933 with a time course similar to that of the fall in BP. These results are consistent with an effect of BHT-933 on BP control through an action on alpha 2-receptors at the level of the brainstem.
我们对一种特定的α2-肾上腺素能受体激动剂BHT-933进行了人体药效学研究。该研究纳入了9名血压正常的男性志愿者，他们每人都随机接受了5毫克BHT-933或安慰剂。BHT-933显著降低了仰卧位和站立位的收缩压和舒张压（BP），给药后3 - 4小时出现最大效果。仰卧位数值：安慰剂组为116/73；BHT-933组为99/64。站立位数值：安慰剂组为114/79；BHT-933组为92/67。即使在血压下降最大时，BHT-933对心率也没有影响。仰卧位时血浆去甲肾上腺素浓度显著降低：安慰剂组为2.5±0.8纳摩尔/升；BHT-933组为1.7±0.6。BHT-933对瓦尔萨尔瓦动作和冷加压试验伴随的血流动力学变化没有影响。所有受试者在服用BHT-933后均出现镇静和口干，其时间进程与血压下降相似。这些结果与BHT-933通过作用于脑干水平的α2受体来控制血压的作用一致。
