Corradi L, Groothold G, Venco A, Mailland F, Negri F, Grandi A, Barzizza F, Finardi G
J Hypertens Suppl. 1986 Dec;4(6):S137-40.
Indenolol is a new antihypertensive agent, whose beta 1-adrenoceptor antagonist properties combined with beta 2-adrenoceptor agonist properties have been shown by experimental studies in animals. Our previous work reported that in vivo beta-adrenoceptor blocking drugs markedly increase the beta-adrenoceptor (BAR) number, without increasing BAR affinity. The aim of this study was to evaluate BAR density and affinity before and after indenolol therapy in membranes of polymorphonucleates (PMN) of patients with essential hypertension. Polymorphonuclear binding parameters were studied in 12 hypertensives (WHO stages I and II) after 14 days of placebo and after 21 days of indenolol therapy (120 mg once daily orally). Indenolol did not increase BAR number but significantly decreased (P less than 0.01) BAR affinity. On the basis of these data it is concluded that indenolol does not induce the same changes in PMN's BAR as previously observed with oxprenolol, propranolol and labetalol. This phenomenon may account for the absence of rebound effect after withdrawal of indenolol in hypertensives.
吲哚洛尔是一种新型抗高血压药物，动物实验研究表明其兼具β1 -肾上腺素能受体拮抗剂特性和β2 -肾上腺素能受体激动剂特性。我们之前的研究报道，体内β -肾上腺素能受体阻断药物可显著增加β -肾上腺素能受体（BAR）数量，但不增加BAR亲和力。本研究旨在评估原发性高血压患者多形核白细胞（PMN）膜在吲哚洛尔治疗前后的BAR密度和亲和力。对12例高血压患者（WHO分级I级和II级）进行研究，在服用安慰剂14天后以及吲哚洛尔治疗21天（每日口服120mg，一次）后，研究多形核白细胞结合参数。吲哚洛尔未增加BAR数量，但显著降低（P＜0.01）BAR亲和力。基于这些数据得出结论，吲哚洛尔在PMN的BAR上不会引起与氧烯洛尔、普萘洛尔和拉贝洛尔之前观察到的相同变化。这种现象可能解释了高血压患者停用吲哚洛尔后无反跳效应的原因。
