Brodde O E, Daul A E, Wang X L, Michel M C, Galal O
Clin Pharmacol Ther. 1987 Apr;41(4):371-9. doi: 10.1038/clpt.1987.43.
We compared the effects of acute stimulation of sympathetic activity by dynamic exercise on a bicycle on lymphocyte beta 2-adrenoceptor density and 10 mumol/L (-)-isoprenaline-evoked lymphocyte cyclic adenosine monophosphate increases in normotensive volunteers with those in patients with essential hypertension. In normotensive subjects exercise increased lymphocyte beta 2-adrenoceptors by about 100%. This effect seems to be a beta 2-dependent process, since it is prevented by propranolol (5 mg administered intravenously) and the beta 2-selective antagonist ICI 118,551 (25 mg t.i.d. orally for 2 weeks) but not by the beta 1-selective antagonist bisoprolol (2.5 mg administered intravenously). In patients with essential hypertension who have elevated lymphocyte beta 2-adrenoceptors, dynamic exercise caused only marginal beta 2-adrenoceptor changes, suggesting an impairment of the acute beta-adrenoceptor regulation. Normalization of blood pressure by antihypertensive treatment resulted in a significant fall in lymphocyte beta 2-adrenoceptors and in a restoration of exercise-induced beta 2-adrenoceptor increases. It is concluded that in essential hypertension the impairment of beta-adrenoceptor regulation is directly linked to the elevated blood pressure.
我们比较了在自行车上进行动态运动对正常血压志愿者和原发性高血压患者淋巴细胞β2 - 肾上腺素能受体密度以及10μmol/L(-)-异丙肾上腺素诱发的淋巴细胞环磷酸腺苷增加的急性交感神经活动刺激作用。在正常血压受试者中,运动使淋巴细胞β2 - 肾上腺素能受体增加约100%。这种作用似乎是一个β2依赖性过程,因为普萘洛尔(静脉注射5mg)和β2选择性拮抗剂ICI 118,551(口服25mg,每日3次,共2周)可阻止其发生,但β1选择性拮抗剂比索洛尔(静脉注射2.5mg)则不能。在淋巴细胞β2 - 肾上腺素能受体升高的原发性高血压患者中,动态运动仅引起β2 - 肾上腺素能受体的微小变化,提示急性β - 肾上腺素能受体调节受损。通过抗高血压治疗使血压正常化导致淋巴细胞β2 - 肾上腺素能受体显著下降,并恢复运动诱导的β2 - 肾上腺素能受体增加。结论是,在原发性高血压中,β - 肾上腺素能受体调节受损与血压升高直接相关。