主要研究目的：按有关生物等效性试验的规定，选择Sanofi Aventis U.S.,LLC为持证商的盐酸决奈达隆片（商品名：迈达龙，规格：400mg）为参比制剂，对石家庄四药有限公司生产的受试制剂盐酸决奈达隆片（规格：400mg）进行餐后给药人体生物等效性试验，比较受试制剂中药物的吸收速度和吸收程度与参比制剂的差异是否在可接受的范围内，评价两种制剂在餐后给药条件下的生物等效性。次要研究目的：观察健康志愿受试者口服受试制剂盐酸决奈达隆片（规格：400mg）和参比制剂盐酸决奈达隆片（商品名：迈达龙，规格：400mg）的安全性。

开始日期2023-11-19

申办/合作机构

石家庄四药有限公司

CTR20233468 / CompletedN/A

盐酸决奈达隆片的人体生物等效性研究

研究空腹/餐后状态下单次口服受试制剂盐酸决奈达隆片与参比制剂盐酸决奈达隆片（迈达龙®）在健康成年男性受试者体内的药代动力学，评价空腹/餐后状态下口服两种制剂的生物等效性和安全性。

开始日期2023-10-25

申办/合作机构

齐鲁制药有限公司

CTR20233080 / CompletedN/A

在中国健康受试者空腹及餐后状态下单次口服盐酸决奈达隆片（规格：400 mg）的人体生物等效性试验

主要目的：评价中国健康受试者空腹及餐后条件下单次口服盐酸决奈达隆片受试制剂（规格：400 mg，生产厂家：江西科睿药业有限公司）和参比制剂（商品名：迈达龙®，规格：400 mg，生产厂家：Sanofi Winthrop Industrie）后的药代动力学特征，考察两制剂在空腹及餐后条件下是否具有生物等效性。次要目的：评价盐酸决奈达隆片受试制剂（规格：400 mg）和参比制剂（商品名：迈达龙®，规格：400 mg）在健康受试者中的安全性。

开始日期2023-10-17

申办/合作机构

江西科睿药业有限公司

100 项与 β1-adrenergic receptor x L-type calcium channel 相关的临床结果

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100 项与 β1-adrenergic receptor x L-type calcium channel 相关的转化医学

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0 项与 β1-adrenergic receptor x L-type calcium channel 相关的专利（医药）

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项与 β1-adrenergic receptor x L-type calcium channel 相关的文献（医药）

2023-12-01·Royal Society Open Science

Potential application of bisoprolol derivative compounds as antihypertensive drugs: synthesis and in silico study

Article

作者: Ivansyah, Atthar Luqman ; Handayani, Nurrahmi ; Saputra, Muhammad Yogi ; Fadylla, Nurdiani ; Oktaviani, Ni Putu Sani ; Wahyuningrum, Deana

Two bisoprolol derivatives, N -acetyl bisoprolol and N -formyl bisoprolol, belonging to the beta-blocker class of antihypertensive drugs, were synthesized using acetylation and formylation reactions. The yields of the reactions were determined to be 32.40% for N -acetyl bisoprolol and 20.20% for N -formyl bisoprolol. In silico methods such as molecular docking, molecular dynamics simulation and SwissADME prediction were employed to evaluate the potential of these bisoprolol derivatives as antihypertensive drugs. These methods were used to assess the interaction between the bisoprolol derivatives and various receptors associated with hypertension, including human angiotensin I-converting enzyme (PDB ID: 1O8A), renin (PDB ID: 2V0Z), beta-1 adrenergic receptors (PDB ID: 4BVN, 7BVQ), voltage-dependent L-type calcium channel subunit alpha-1S (PDB ID: 6JP5) and mineralocorticoid receptor (PDB ID: 6L88). Our results demonstrated the highest binding energy when bisoprolol and its derivatives bound to 4BVN, with binding energy values of 6.74 kcal mol −1 , 7.03 kcal mol −1 and 7.63 kcal mol −1 for bisoprolol, N -acetyl bisoprolol and N -formyl bisoprolol, respectively. The stability of these complexes was confirmed by molecular dynamics simulations, with a root-mean-square deviation value of approximately 2. Furthermore, the SwissADME results indicated that both derivatives exhibited similar properties to the reference drug bisoprolol.

2023-10-01·Journal of traditional Chinese medicine = Chung i tsa chih ying wen pan

Mechanism of Lingbao Huxin Dan in the treatment of bradyarrhythmia complicated with coronary heart disease: a network pharmacology analysis.

Article

作者: Huagang, Han ; Junling, Cao ; Tianquan, Wang ; Lingyan, Dong ; Ziqiang, L I ; Jingfeng, Ouyang

OBJECTIVETo investigate the mechanism of action of the Lingbao Huxin Dan in treating bradycardia arrhythmia with coronary heart disease (BA-CHD) by network pharmacology.METHODSThe active ingredients of the Lingbao Huxin Dan were screened on the Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform and Bioinformatics tools designed for the analysis of molecular mechanisms of Chinese medicine platform; target prediction was conducted with the SwissTargetPrediction database, and Cytoscape 3.8 was used to construct a drug ingredient-target network. The Genecards, Online Mendelian Inheritance in Man, and DrugBank databases were searched for disease targets. Venn plots were used to display the common targets of BA-CHD and active ingredients. The STRING platform was used to construct a protein-protein interaction network. The Metascape data platform was used for Gene Ontology (GO) enrichment analysis and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis to construct a signaling pathway network of the active ingredients of the Lingbao Huxin Dan.RESULTSThere were 121 active ingredients, 899 related targets, 39 targets important in BA-CHD and 14 targets which intersected between the active ingredients and BA-CHD. There were 27 core therapeutic ingredients, 153 biological processes, 18 cell ingredients and 20 molecular functions obtained by GO enrichment analysis. The KEGG pathway analysis yielded 19 signaling pathways.CONCLUSIONRBA-CHD may treat BA-CHD by regulating adrenergic receptor beta-1, alpha 1-α adrenergic receptor, calcium voltage-gated channel subunit alpha1 C, alpha-1β-adrenergic receptor, nitric oxide synthase 2, beta-2 adrenergic receptor, voltage-dependent calcium channel subunit alpha-2/delta-1, an- giotensin-converting enzyme, Raf-1 proto-oncogene serine/threonine-protein kinase, and other targets, potentially by affecting adrenergic receptor binding and calcium channel opening, to regulate the activity of cardiomyocytes.

2020-04-24·Circulation Journal3区 · 医学

Cardiac Arrhythmias in Autoimmune Diseases

3区 · 医学

Review

作者: Kosiuk, Jędrzej ; Gawałko, Monika ; Lodziński, Piotr ; Balsam, Paweł ; Grabowski, Marcin ; Krzowski, Bartosz ; Opolski, Grzegorz

Autoimmune diseases (ADs) affect approximately 10% of the world's population. Because ADs are frequently systemic disorders, cardiac involvement is common. In this review we focus on typical arrhythmias and their pathogenesis, arrhythmia-associated mortality, and possible treatment options among selected ADs (sarcoidosis, systemic lupus erythematosus, scleroderma, type 1 diabetes, Graves' disease, rheumatoid arthritis, ankylosing spondylitis [AS], psoriasis, celiac disease [CD], and inflammatory bowel disease [IBD]). Rhythm disorders have different underlying pathophysiologies; myocardial inflammation and fibrosis seem to be the most important factors. Inflammatory processes and oxidative stress lead to cardiomyocyte necrosis, with subsequent electrical and structural remodeling. Furthermore, chronic inflammation is the pathophysiological basis linking AD to autonomic dysfunction, including sympathetic overactivation and a decline in parasympathetic function. Autoantibody-mediated inhibitory effects of cellular events (i.e., potassium or L-type calcium currents, M₂muscarinic cholinergic or β₁-adrenergic receptor signaling) can also lead to cardiac arrhythmia. Drug-induced arrhythmias, caused, for example, by corticosteroids, methotrexate, chloroquine, are also observed among AD patients. The most common arrhythmia in most AD presentations is atrial arrhythmia (primarily atrial fibrillation), expect for sarcoidosis and scleroderma, which are characterized by a higher burden of ventricular arrhythmia. Arrhythmia-associated mortality is highest among patients with sarcoidosis and lowest among those with AS; there are scant data related to mortality in patients with psoriasis, CD, and IBD.