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 ADRA1 x VDCCs 相关的临床结果

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100 项与 ADRA1 x VDCCs 相关的转化医学

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0 项与 ADRA1 x VDCCs 相关的专利（医药）

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项与 ADRA1 x VDCCs 相关的文献（医药）

2024-02-01·Biochemical and Biophysical Research Communications

Subcellular localization and ER-mediated cytotoxic function of α1A and α1ACT in spinocerebellar ataxia type 6

Article

作者: Honda, Shinya ; Shimizu, Shigeomi ; Mizusawa, Hidehiro ; Shin, Min Kyoung ; Watase, Kei ; Wang, Di ; Ishikawa, Kinya

Spinocerebellar ataxia type 6 (SCA6) is a polyglutamine (polyQ) disease, which is caused by the elongation of CAG repeats encoding polyQ in the CACNA1A gene. The CACNA1A gene encodes two proteins, namely, α1A (a subunit of the plasma membrane calcium channel), which is translated in its entire length, and α1ACT, which is translated from the second cistron, and both proteins have a polyQ tract. The α1A-polyQ and α1ACT-polyQ proteins with an elongated polyQ stretch have been reported to form aggregates in cells and induce neuronal cell death, but the subcellular localization of these proteins and their cytotoxic properties remain unclear. In this study, we first analyzed SCA6 model mice and found that α1A-polyQ^long localized mainly to the Golgi apparatus, whereas a portion of α1ACT-polyQ^long localized to the nucleus. Analysis using Neuro2a cells also showed similar subcellular localizations of these proteins, and a proportion of both proteins localized to the endoplasmic reticulum (ER). Cytotoxic studies demonstrated that both proteins induce both the ER stress response and apoptosis, indicating that they are able to induce ER stress-induced apoptosis.

2023-10-01·Journal of Pharmacological Sciences

Pimaric acid reduces vasoconstriction via BKCa channel activation and VDCC inhibition in rat pulmonary arterial smooth muscles

Article

作者: Ota, Mina ; Yamamura, Hisao ; Amano, Taiki ; Kondo, Rubii ; Hikawa, Yukari ; Imaizumi, Yuji ; Fujiwara, Moe ; Suzuki, Yoshiaki ; Yamamura, Aya ; Ishida, Masashi

Pulmonary vessels play a pivotal role in oxygen circulation. We previously demonstrated that pimaric acid (PiMA) activated large-conductance Ca²⁺-activated K⁺ (BK_Ca) channels and inhibited voltage-dependent Ca²⁺ channels (VDCCs). In the present study, PiMA attenuated vasoconstriction induced by high K⁺ or endothelin-1 in rat pulmonary arterial smooth muscles (PASMs). PiMA also reduced high K⁺-induced cytosolic [Ca²⁺] increase in PASM cells. PiMA increased BK_Ca currents and decreased VDCC currents. BK_Ca channels and VDCCs were formed by the α/β₁ and α_1C/α_1D/β₂/β₃ subunits, respectively. These results indicate that PiMA induces vasorelaxation through the dual effects of BK_Ca channel activation and VDCC inhibition in PASMs.

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.