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揭示雷诺嗪在抗心绞痛药物应用之外的药理和治疗潜力:新见解

Unraveling the pharmacological and therapeutic potential of Ranolazine beyond antianginal drug use: a new insight.

作者信息

Singh Dhirendra, Oladimeji-Salami Joy Awulika, Akindele Abidemi James

机构信息

Department of Pharmacology, M.M College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Mullana, Ambala, Haryana, India.

Special Duties Department, National Biotechnology Development Agency, Abuja, Nigeria.

出版信息

Exp Biol Med (Maywood). 2025 Sep 3;250:10604. doi: 10.3389/ebm.2025.10604. eCollection 2025.

Abstract

Ranolazine (RAN) is an acetanilide and piperazine derivative that selectively blocks the late sodium current in cardiac cells and is prescribed in adults as an add-on medication for the symptomatic management of patients with stable angina pectoris who are insufficiently managed or intolerant of first-line antianginal treatments. RAN was first approved by the U.S. Food and Drug Administration (FDA) in 2006 and the European Medicine Agency in 2008 for the treatment of chronic stable angina. RAN has no substantial effect on hemodynamic indicators, including heart rate and blood pressure. RAN also slows fatty acid oxidation, which increases glucose oxidation, lowers lactic acid generation, and optimizes heart performance. Besides its antianginal effect, RAN has recently revealed additional pharmacological properties such as neuroprotective, hepatoprotective, renal protective, cardioprotective, and antidiabetic effects and other beneficial pharmacological activities. We choose to write this current review paper to address the many hidden pharmacological and therapeutic potentials of RAN beyond its antianginal activity.

摘要

雷诺嗪(RAN)是一种乙酰苯胺和哌嗪衍生物,可选择性阻断心肌细胞的晚钠电流,在成人中作为附加药物用于症状性治疗稳定型心绞痛患者,这些患者对一线抗心绞痛治疗管理不足或不耐受。RAN于2006年首次获得美国食品药品监督管理局(FDA)批准,并于2008年获得欧洲药品管理局批准用于治疗慢性稳定型心绞痛。RAN对包括心率和血压在内的血流动力学指标没有实质性影响。RAN还可减缓脂肪酸氧化,从而增加葡萄糖氧化,降低乳酸生成,并优化心脏功能。除了其抗心绞痛作用外,RAN最近还显示出其他药理特性,如神经保护、肝保护、肾保护、心脏保护和抗糖尿病作用以及其他有益的药理活性。我们选择撰写这篇综述文章,以探讨RAN除抗心绞痛活性之外的许多潜在药理和治疗潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/10dc/12440829/2317cc005fee/EBM_ebm-2025-10604_wc_abs.jpg

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