**Background**
Hypertension and angina pectoris are prevalent cardiovascular conditions characterized by elevated blood pressure and reduced myocardial oxygen supply, respectively. These conditions often lead to severe complications, including myocardial infarction and heart failure, making the regulation of the adrenergic system a primary therapeutic target. The β1-adrenergic receptor plays a critical role in modulating heart rate and contractility; therefore, selective blockade of this receptor can effectively reduce cardiac workload and stabilize blood pressure. In this context, we will introduce a cardioselective β1-adrenergic receptor blocker – Atenolol.
**Definition**
Atenolol is a cardioselective β1-adrenergic receptor blocker with a Ki of 697 nM at the β1-adrenoceptor in guinea pig left ventricle membrane. According to the Atenolol technical information, it is used extensively in the research of hypertension and angina pectoris.
**In Vitro and In Vivo Studies**
The Atenolol biological activity has been demonstrated across various experimental models. In vitro studies indicate that Atenolol (1-100 μM, 5 h) strengthens the inhibitory effect on the migration of rat aortic smooth muscle cells when combined with Nifedipine (1-100 μM). Furthermore, Atenolol (1-100 μM) inhibited cell proliferation in rat aortic smooth muscle cells, with a 20% reduction observed after 72 h of incubation at 100 μM. In hemangioma-derived endothelial cells (Hem-ECs), Atenolol (50-150 μM, 24 h) decreased cell survival in a dose-dependent manner. Notably, research into Atenolol Autophagy showed that treatment with 100 μM for 6 h increased the LC3-Ⅱ/LC3-Ⅰ ratio and decreased p62 in Hem-ECs.
Atenolol in vivo studies have further validated its efficacy. In 2K1C renovascular hypertensive rats, the combination of Atenolol (5-20 mg/kg, i.g., single dose) and Amlodipine reduced and stabilized blood pressure within 24 h. In an Hras5 tumor xenograft rat model, Atenolol (6 mg/kg, p.o., single dose) combined with Nifedipine abolished the hypertensive and tachycaidic effects induced by ZD6126. Additionally, chronic administration of Atenolol (40 mg/kg, p.o., daily for 6 weeks) in male Wistar rats increased the density of plasma membrane β1- and β2-adrenoceptors while decreasing β1-adrenoceptor mRNA expression. In conclusion, Atenolol is a potent cardioselective β1-blocker effective for modulating cardiovascular function and cell behavior.
Keywords
Atenolol, 29122-68-7, (RS)-Atenolol, Adrenergic Receptor, Beta Receptor, Hypertension, angina pectoris, β1-adrenergic receptor, cardioselective, Hem-ECs, Inhibitor, inhibitor, inhibit
References
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