更新于：2024-11-01

ACE x ADRA1 x β2-adrenergic receptor x β1-adrenergic receptor

更新于：2024-11-01

基本信息

关联

项与 ACE x ADRA1 x β2-adrenergic receptor x β1-adrenergic receptor 相关的药物

Carvedilol/Lisinopril

卡维地洛/赖诺普利

靶点

ACE x ADRA1 x β1-adrenergic receptor x β2-adrenergic receptor

作用机制

ACE抑制剂 [+3]

在研机构-

原研机构

GSK Plc

在研适应症-

非在研适应症

高血压

最高研发阶段终止

首次获批国家/地区-

首次获批日期1800-01-20

项与 ACE x ADRA1 x β2-adrenergic receptor x β1-adrenergic receptor 相关的临床试验

NCT00624065 / Completed临床3期

COR111096, A Randomized, Double-Blind, Active-Controlled, Parallel Group, Multicenter Study Comparing the Proportion of Subjects With Stage 1 or 2 Essential Hypertension Who Achieve Target Blood Pressure While Receiving Either Carvedilol CR + Lisinopril or Lisinopril Monotherapy

Randomized, double-blind, parallel group, multicenter study of subjects with Stage 1 or 2 essential hypertension who are not at target blood pressure (<140/90mmHg) at Baseline. Subjects will be randomized to receive either carvedilol CR + lisinopril or lisinopril + placebo. Subjects will be uptitrated over a 6 week period until target blood pressure (<140/90mmHg) is met. The primary objective of the study is to compare the proportion of subjects who achieve target blood pressure after 6 weeks of treatment.

开始日期2008-03-01

申办/合作机构

GSK Plc

100 项与 ACE x ADRA1 x β2-adrenergic receptor x β1-adrenergic receptor 相关的临床结果

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100 项与 ACE x ADRA1 x β2-adrenergic receptor x β1-adrenergic receptor 相关的转化医学

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0 项与 ACE x ADRA1 x β2-adrenergic receptor x β1-adrenergic receptor 相关的专利（医药）

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项与 ACE x ADRA1 x β2-adrenergic receptor x β1-adrenergic receptor 相关的文献（医药）

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.

2004-01-01·Hypertension Research3区 · 医学

The Thiazide-Sensitive Na+-Cl- Cotransporter Gene, C1784T, and Adrenergic Receptor-β3 Gene, T727C, May Be Gene Polymorphisms Susceptible to the Antihypertensive Effect of Thiazide Diuretics

3区 · 医学

Article

作者: Kei Kamide ; Hajime Nakahama ; Satoko Nakamura ; Fumiki Yoshihara ; Tetsutaro Matayoshi ; Yoshikazu Miwa ; Mariko Banno ; Shin Takiuchi ; Takeshi Horio ; Masayoshi Yoshii ; Yuhei Kawano ; Toshiyuki Miyata ; Yoichi Takami ; Chihiro Tanaka ; Takashi Inenaga

The response of blood pressure to thiazide diuretics (TZDs) differs among individuals. The prediction of the antihypertensive effect of TZDs is important for realizing individualized therapy in the management of hypertension. The aim of this study was to identify the single nucleotide polymorphisms (SNPs) susceptible to the antihypertensive effect of TZDs, particularly focusing on genes related to water-electrolyte absorption in the kidney. Seventy-six outpatients (mean age, 65.4+/-9.0 years) with essential hypertension (EHT) taking TZDs were retrospectively assessed. We defined as responders (R) those whose mean blood pressure was lowered by more than 5 mmHg after the use of TZDs. Forty-eight SNPs in 17 genes (ADD1, GNB3, TSC [SLC12A3], MLR [NR3C2], NCX1 [SLC8A1], WNK1, WNK4, AGT, ACE, AT1 [AGTR1], CYP11B2, ADRB1, ADRB2, ADRB3, ADRA1A, ADRA1B, ADRA2A) were genotyped in the 76 patients. The SNPs in TSC, MLR, NCX1, WNK1, and WNK4 were identified by direct sequencing and those with minor frequencies of greater than 5% were genotyped in this study. The comparison of polymorphism prevalence between R and non-responders (NR) showed significant differences in TSC C1784T (C allele vs. T allele, odds ratio (OR)=3.81, p =0.016, confidence interval (CI): 1.25-11.63) and ADRB3 T727C (Trp64Arg) (T allele vs. C allele, OR=4.59, p =0.005, CI: 1.54-13.68). The blood pressure (BP) in patients homozygous for the major alleles of both TSC C1784T and ADRB3 T727C were significantly reduced by TZD treatment; however, the BP in those homozygous for the minor allele and heterozygous (TSC C1784T: TT+CT; ADRB3 T727C: CC+CT) for both SNPs were not significantly changed after TZD treatment. Both newly detected TSC C1784T and ADRB3 T727C are gene polymorphisms susceptible to the antihypertensive effect of TZDs in patients with EHT. Thus, the prediction of BP reduction by TZDs may be possible by evaluating these two SNPs.