Fontaine Rebecca L, Brooks Daniel J, Barlow Deborah, Neilson Ryan J, Lary Christine W, Houseknecht Karen L, Motyl Katherine J
Center for Molecular Medicine, MaineHealth Institute for Research, MaineHealth, Scarborough, ME, 04074, United States.
Graduate School of Biomedical Science and Engineering, University of Maine, Orono, ME, 04469, United States.
JBMR Plus. 2025 May 15;9(7):ziaf087. doi: 10.1093/jbmrpl/ziaf087. eCollection 2025 Jul.
Atenolol is a β1-selective β-adrenergic receptor antagonist (a.k.a. β-blocker) and is under investigation in a clinical trial to prevent osteoporosis in postmenopausal women. The effects of atenolol on rodent bone are unknown, which limits research investigating mechanisms or modeling human treatment effects. However, propranolol, a non-selective β-blocker, has been widely used in rodent models. Propranolol co-treatment with intermittent truncated PTH improves a serum marker of bone formation, P1NP, while blocking the PTH-induced increase in CTX-I-MMP, a serum marker of bone resorption. To determine whether atenolol has similar properties as propranolol during co-treatment, we tested the combined effects of atenolol and PTH in female C57BL/6J mice. Atenolol exposure was confirmed in both serum and marrow at clinically relevant levels. Atenolol had little effect on femoral or L5 vertebra microarchitecture, either on its own or in combination with PTH, which improved trabecular microarchitecture as expected. However, co-treatment with PTH significantly increased P1NP levels past that of PTH alone, suggesting longer treatment may improve bone density by increasing bone formation. In summary, we found little effect of atenolol alone or in combination with PTH, which may be related to relative selectivity of atenolol for β1AR over β2AR, the predominant βAR in bone. Future studies should test whether longer term atenolol may improve microarchitectural parameters with PTH co-treatment.
阿替洛尔是一种β1选择性β肾上腺素能受体拮抗剂(又名β阻滞剂),目前正在一项临床试验中进行研究,以预防绝经后女性的骨质疏松症。阿替洛尔对啮齿动物骨骼的影响尚不清楚,这限制了对其作用机制或人类治疗效果建模的研究。然而,非选择性β阻滞剂普萘洛尔已广泛应用于啮齿动物模型。普萘洛尔与间歇性截短的甲状旁腺激素(PTH)联合治疗可改善骨形成的血清标志物P1NP,同时阻断PTH诱导的骨吸收血清标志物CTX-I-MMP的增加。为了确定阿替洛尔在联合治疗期间是否具有与普萘洛尔相似的特性,我们在雌性C57BL/6J小鼠中测试了阿替洛尔和PTH的联合作用。在血清和骨髓中均证实了阿替洛尔在临床相关水平的暴露。阿替洛尔单独使用或与PTH联合使用时,对股骨或L5椎骨的微结构几乎没有影响,而PTH联合使用时可如预期改善小梁微结构。然而,与PTH联合治疗显著提高了P1NP水平,超过了单独使用PTH时的水平,这表明更长时间的治疗可能通过增加骨形成来提高骨密度。总之,我们发现阿替洛尔单独使用或与PTH联合使用时几乎没有效果,这可能与阿替洛尔对β1肾上腺素能受体(β1AR)相对于β2肾上腺素能受体(β2AR)的相对选择性有关(β2AR是骨骼中主要的β肾上腺素能受体)。未来的研究应测试长期使用阿替洛尔与PTH联合治疗是否可改善微结构参数。