Ziegler M G, Chernow B, Woodson L C, Coyle J, Cruess D, Lake C R
Clin Pharmacol Ther. 1986 Jul;40(1):116-9. doi: 10.1038/clpt.1986.147.
Normal subjects given propranolol increased their plasma t1/2 for infused isoproterenol from 2.68 to 6.25 minutes. Propranolol increased plasma norepinephrine (NE) levels only slightly. Propranolol increased the t1/2 of isoproterenol but not that of NE in men with autonomic nervous system degeneration. This suggests that propranolol acts on nonneuronal uptake-2 processes, rather than on uptake-1 mechanisms. alpha-Blockers slow uptake-1 and beta-blockers slow uptake-2 processes. When 27 subjects exercised, those who attained the highest plasma levels of the alpha- and beta-receptor agonist NE also had the briefest apparent t1/2 for NE. Adrenergic receptor blocking drugs slow catecholamine clearance. NE may stimulate its own clearance.
给予普萘洛尔的正常受试者,其输注异丙肾上腺素后的血浆半衰期从2.68分钟延长至6.25分钟。普萘洛尔仅使血浆去甲肾上腺素(NE)水平略有升高。在自主神经系统退化的男性中,普萘洛尔延长了异丙肾上腺素的半衰期,但未延长NE的半衰期。这表明普萘洛尔作用于非神经元摄取-2过程,而非摄取-1机制。α受体阻滞剂减慢摄取-1过程,β受体阻滞剂减慢摄取-2过程。27名受试者运动时,血浆中α和β受体激动剂NE水平最高的受试者,其NE的表观半衰期也最短。肾上腺素能受体阻断药物减慢儿茶酚胺清除。NE可能刺激其自身清除。