二乙脲心安可作为治疗轻及中度高血压的第一线药物。它是一种无膜稳定作用的心脏选择性β受体阻滞药,对β_1肾上腺素能受体具有高度的选择性。取鼠心膜(β_1受体)和网状内皮细胞(β_2受体)进行放射配体结合研究,发现该药首先与β_1受体结合。二乙脲心安还具有部分激动β_2受体和微弱阻滞α_2肾上腺能受体的作用。部分β_2肾上腺素能受体激动作用表现为:该药使人体白细胞上β_2受体密度减少30％。该药对哮喘患者几乎不引起支气管收缩。研究表明二乙脲心安能直接扩张周围血管。对高血压病人进行双盲交叉研究,比较二乙脲心安(200～400mg每天一次)与美托洛尔(100～200mg每天一 Dimethylurea may be the first line of treatment for mild and moderate hypertension. It is a cardioselective β-blocker with no membrane stabilization and is highly selective for β 1 -adrenoceptors. Radioligand binding studies were performed with rat cardiac membrane (β 1 receptor) and reticuloendothelial cells (β 2 receptor) and found that this drug first binds to the β 1 receptor. Diethylurea also has partial agonism of β 2 receptor and weak block α 2 adrenergic receptor role. Partial β_2 adrenergic receptor agonism is manifested as: The drug reduces the density of β 2 receptors on human leukocytes by 30%. This medicine causes almost no bronchoconstriction in patients with asthma. Studies show that diethylurea cardiorespiratory direct expansion of peripheral blood vessels. A double-blind crossover study of hypertensive patients was performed to compare the efficacy of diethylurea (200-400 mg once daily) with metoprolol (100-200 mg daily