Higenamine
(Synonyms: 去甲乌药碱; Norcoclaurine) 目录号 : GC38099
Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
Cas No.:5843-65-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Demethyl-Coclaurine (Higenamine, Norcoclaurine), the key component of the Chinese herb aconite root, is a beta-2 adrenergic receptor (β2-AR) agonist. Demethyl-Coclaurine stimulates AKT phosphorylation and requires PI3K activation for the anti-apoptotic effect in cardiomyocytes.
[1] Sang-Rok Lee, et al. Lipids Health Dis. 2013 Oct 21;12:148. [2] Mei-ping Wu, et al. Pharmacol Res. 2016 Feb;104:115-23.
| Cas No. | 5843-65-2 | SDF | |
| 别名 | 去甲乌药碱; Norcoclaurine | ||
| Canonical SMILES | OC1=CC2=C(C(CC3=CC=C(O)C=C3)NCC2)C=C1O | ||
| 分子式 | C16H17NO3 | 分子量 | 271.31 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.6858 mL | 18.4291 mL | 36.8582 mL |
| 5 mM | 0.7372 mL | 3.6858 mL | 7.3716 mL |
| 10 mM | 0.3686 mL | 1.8429 mL | 3.6858 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Higenamine in Plants as a Source of Unintentional Doping
Plants (Basel) 2022 Jan 27;11(3):354.PMID:35161335DOI:10.3390/plants11030354.
Background: Higenamine is a β2 agonist of plant origin. The compound has been included in WADA's prohibited list since 2017. Higenamine may be detected in different plants and many food supplements of natural origin. Methods: Our literature search was conducted through PubMed, Science Direct, Google Scholar, and Web of Science studies investigating the presence of Higenamine in plants that are used in traditional folk medicine or included in food supplements. Our study aimed to assess the risk of adverse analytical findings caused by higenamine-containing plants. Results: Based on our literature search, Nelumbo nucifera, Tinospora crispa, Nandina domestica, Gnetum parvifolium, Asarum siebodii,Asarum heterotropoides, Aconitum carmichaelii, and Aristolochia brasiliensis are higenamine-containing plants. Based on data from Eastern folk medicine, these plants can provide numerous health benefits. Professional athletes likely ingest these plants without knowing that they contain Higenamine; these herbs are used in treatments for different conditions and various foods/food supplements in addition to folk medicine. Conclusion: Athletes and their teams must be aware of the issues associated with the use of plant-based products. They should avoid consuming higenamine-containing plants during and outside of competition periods.
Role of Higenamine in Heart Diseases: A Mini-Review
Front Pharmacol 2022 Jan 10;12:798495.PMID:35082678DOI:10.3389/fphar.2021.798495.
Higenamine, a natural product with multiple targets in heart diseases, is originally derived from Aconitum, which has been traditionally used in China for the treatment of heart disease, including heart failure, arrhythmia, bradycardia, cardiac ischemia/reperfusion injury, cardiac fibrosis, etc. This study is aimed to clarify the role of Higenamine in heart diseases. Higenamine has effects on improving energy metabolism of cardiomyocytes, anti-cardiac fibroblast activation, anti-oxidative stress and anti-apoptosis. Accumulating evidence from various studies has shown that Higenamine exerts a wide range of cardiovascular pharmacological effects in vivo and in vitro, including alleviating heart failure, reducing cardiac ischemia/reperfusion injury, attenuating pathological cardiac fibrosis and dysfunction. In addition, several clinical studies have reported that Higenamine could continuously increase the heart rate levels of healthy volunteers as well as patients with heart disease, but there are variable effects on systolic blood pressure and diastolic blood pressure. Moreover, the heart protection and therapeutic effects of Higenamine on heart disease are related to regulating LKB1/AMPKα/Sirt1, mediating the β2-AR/PI3K/AKT cascade, induction of heme oxygenase-1, suppressing TGF-β1/Smad signaling, and targeting ASK1/MAPK (ERK, P38)/NF-kB signaling pathway. However, the interventional effects of Higenamine on heart disease and its underlying mechanisms based on experimental studies have not yet been systematically reviewed. This paper reviewed the potential pharmacological mechanisms of Higenamine on the prevention, treatment, and diagnosis of heart disease and clarified its clinical applications. The literature shows that Higenamine may have a potent effect on complex heart diseases, and proves the profound medicinal value of Higenamine in heart disease.
β2 -Adrenoceptor agonist activity of Higenamine
Drug Test Anal 2021 Feb;13(2):261-267.PMID:33369180DOI:10.1002/dta.2992.
Higenamine was included in the World Anti-Doping Agency (WADA) Prohibited Substances and Methods List as a β2 -adrenoceptor agonist in 2017, thereby resulting in its prohibition both in and out of competition. The present mini review describes the physiology and pharmacology of adrenoceptors, summarizes the literature addressing the mechanism of action of Higenamine and extends these findings with previously unpublished in silico and in vitro work. Studies conducted in isolated in vitro systems, whole-animal preparations and a small number of clinical studies suggest that Higenamine acts in part as a β2 -adrenoceptor agonist. In silico predictive tools indicated that Higenamine and possibly a metabolite have a high probability of interacting with the β2 -receptor as an agonist. Stable expression of human β2 -receptors in Chinese hamster ovary (CHO) cells to measure agonist activity not only confirmed the activity of Higenamine at β2 but also closely agreed with the in silico prediction of potency for this compound. These data confirm and extend literature findings supporting the inclusion of Higenamine in the Prohibited List.
Applications of Higenamine in pharmacology and medicine
J Ethnopharmacol 2017 Jan 20;196:242-252.PMID:28007527DOI:10.1016/j.jep.2016.12.033.
Ethnopharmacological relevance: Aconitum has been used as local and traditional medicines in many asian regions for the treatment of various diseases such as collapse, syncope, painful joints, oedema, bronchial asthma et al. Higenamine, a plant-based alkaloid, was initially isolated from Aconitum and identified as the active cardiotonic component of Aconitum. It has been tested as a candidate of pharmacologic stress agent in the detection of coronary artery diseases (CADs) and now researchers have just accomplished the phase III clinical studies successfully in China. Besides, a large number of studies have revealed the various pharmacological properties and potentially multi-spectral medical applications of Higenamine. However, to date, no comprehensive review on Higenamine has been published. Aim of the review: This present paper aims to compile a comprehensive update regarding the biochemistry, pharmacokinetic features, pharmacological activities, clinical and potential clinical uses and toxicities on Higenamine with the ultimate objective of providing a guide for future research on this drug. Materials and methods: The selection of relevant data was made through a search using the keyword "Higenamine" in "Web of science", "Pubmed", and "China Knowledge Resource Integrated (CNKI)". Information was also acquired from local classic herbal literature, government reports and conference papers. Results: In addition to Aconitum, Higenamine also exists in many other plants including Tinospora crispa, Nandina domestica THUNBERG, Gnetum Parvifolium C.Y. Cheng, sarum Heterotropoides,Nelumbo nucifera,N.nucifera. The pharmacokinetic studies conducted in animals and humans showed that Higenamine conformed to a two-compartment pharmacokinetic model. Studies over the last four decades on Higenamine have revealed its various pharmacological properties such as positive inotropic and chronotropic effect, activating slow channel effect, vascular and tracheal relaxation effect, anti-thrombotic, anti-apoptotic and anti-oxidative effect, anti-inflammatory and immunomodulatory effect. This phytochemical constituent has shown its potential therapeutic effects for diseases like heart failure, disseminated intravascular coagulation (DIC), shock, arthritis, asthma, ischemia/reperfusion (I/R) injuries and erectile dysfunction. Conclusions: Extensive basic and clinical studies on Higenamine showed valuable therapeutic effects on different disorders. However, the underlying mechanisms of Higenamine have not been established. Therefore, the safety, tolerability and efficacy of Higenamine are as yet, not fully understood. Additionally, some of the studies were small sample-sized and unreliable. To sum up, there is a need for deeper investigation in the mechanisms of Higenamine action, as well as well-designed preclinical and clinical trials studies to test the safety and clinical value of the drug.
Higenamine as a Potential Pharmacologic Stress Agent in the Detection of Coronary Artery Disease
Chin Med Sci J 2022 Sep 30;37(3):275-281.PMID:36321183DOI:10.24920/003936.
Myocardial perfusion imaging (MPI) is valuable for the diagnosis, prognosis, and management of coronary artery disease (CAD). The most commonly used pharmacologic stress agents at present are vasodilators and adrenergic agents. However, these agents have contraindications and may cause adverse effects in some patients. Thus, other stress agents feasible for more patients are required. Higenamine (HG) is a β-adrenergic receptor agonist currently approved for clinical trials as a stress agent for myocardial infarction. It also has a promising value in MPI for the detection of CAD in preclinical and clinical studies. This review summarizes the application of HG on MPI, including its mechanism of action, stress protocol, efficacy, and safety.