Delving into the Latest Updates on Higenamine Hydrochloride with Synapse

Overview

Basic Info

Drug Type

Small molecule drug, Other diagnostic agent

Synonyms-

Target

β2-adrenergic receptor

Mechanism

β2-adrenergic receptor agonists(Beta-2 adrenergic receptor agonists)

Therapeutic Areas

Other DiseasesCardiovascular Diseases

Active Indication

Contrast agentsCoronary Artery Disease

Inactive Indication-

Originator Organization

Zhuhai Rundu Pharmaceutical Co., Ltd.

Active Organization

Zhuhai Rundu Pharmaceutical Co., Ltd.

Institute of Materia Medica

Guangdong South China New Drug Creation Center

+ [1]

Inactive Organization

Chinese Academy of Medical Sciences

Fuwai Cardiovascular Hospital

Drug Highest PhaseNDA/BLA

First Approval Date-

RegulationSpecial Review Project (CN)

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Structure/Sequence

Molecular FormulaC16H17NO3

InChIKeyWZRCQWQRFZITDX-UHFFFAOYSA-N

CAS Registry5843-65-2

View All Structures (2)

将盐酸去甲乌药碱注射液及腺苷注射液作为心脏负荷药物用于核素心肌灌注显像诊断冠心病的结果，分别与冠状动脉造影（金标准）的结果相比较，计算盐酸去甲乌药碱注射液与腺苷注射液诊断冠心病的敏感性，并基于敏感性评估盐酸去甲乌药碱注射液与腺苷注射液的非劣效关系，最终为药物注册申请提供充分的依据。

[Translation]

The results of using higenamine hydrochloride injection and adenosine injection as cardiac stress drugs for radionuclide myocardial perfusion imaging in the diagnosis of coronary heart disease were compared with the results of coronary angiography (gold standard), and the sensitivity of higenamine hydrochloride injection and adenosine injection in diagnosing coronary heart disease was calculated. The non-inferiority relationship between higenamine hydrochloride injection and adenosine injection was evaluated based on the sensitivity, ultimately providing sufficient basis for drug registration applications.

Start Date10 May 2021

Sponsor / Collaborator

Guangdong South China New Drug Creation Center

[+3]

NCT01451229

/ CompletedPhase 1IIT

An Open-Label, Single-dose Administration Study of the Pharmacokinetics and Pharmacodynamics of Higenamine, Administered Intravenously Injection to Healthy Chinese Subjects

The purpose of this study is to assess the pharmacokinetics and pharmacodynamics of higenamine in healthy Chinese subjects

Start Date01 Jun 2009

Sponsor / Collaborator

Peking Union Medical College Hospital

100 Clinical Results associated with Higenamine Hydrochloride

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100 Translational Medicine associated with Higenamine Hydrochloride

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100 Patents (Medical) associated with Higenamine Hydrochloride

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159

Literatures (Medical) associated with Higenamine Hydrochloride

01 Apr 2025·Spectrochimica Acta Part A: Molecular and Biomolecular Spectroscopy

Raman spectroscopic fingerprinting for the identification and quantitative analysis of sports doping β − agonists based on gold nanopolyhedra

Article

Author: Zhang, Yahui ; Tan, Rui ; Zeng, Xuanjiang ; Wang, Chuanfeng ; Li, Ting ; Luo, Xiaojun ; Lin, Ruxi ; Chen, Liping

Beta - stimulant, that is, β - adrenergic stimulant, also known as β - agonists, is bioactive catecholamine compounds naturally produced in animals' adrenal medulla glands that induce relaxation in asthmatic airway smooth muscles upon inhalation while also temporarily boosting athletic alertness and alleviating fatigue. However, their potential for dependency poses health risks including unnoticed exacerbation leading to severe illness or fatality prompting their inclusion on WADA's prohibited substances list. Surface - enhanced Raman spectroscopy (SERS) offers a rapid, sensitive, and label - free means for identifying characteristic peaks associated with β - agonist compounds. In our investigation, the utilization of seed - mediated synthesis technique facilitated production of gold polyhedral substrates serving as highly sensitive biosensors for detecting β - agonist presence. The unique geometry of these particles generates enhanced SERS signals due to their multiple corners, resulting low detection limits (9.33 × 10^-7, 6.28 × 10^-7, and 6.19 × 10^-7 g·mL^-1 for salbutamol, clenbuterol and higenamine respectively), with promising prospects for improving overall sensitivity in β - agonists detection.

01 Mar 2025·Journal of Pharmaceutical and Biomedical Analysis

Evidence for the metabolic activation of higenamine to quinone methide and ortho-quinone metabolites in vitro and in vivo using liquid chromatography tandem mass spectrometry

Article

Author: Wang, Hui ; Hou, Pengyi ; Wang, Wei ; Xin, Lihua ; Sun, Shiwei ; Zheng, Jiang

Higenamine (HG), a naturally occurring benzyltetrahydroisoquinoline alkaloid, has been revealed a variety of biological activities and is extensively utilized in dietary supplements. Currently, HG is under investigation in phase I clinical trials, however, the liver metabolism of HG has so far not been fully elucidated. The present study aimed to identify reactive metabolites of HG using ultrahigh-performance liquid chromatography-tandem mass spectrometry. Four glutathione (GSH) conjugates (M1-M4) and four cysteine conjugates (M5-M8) derived from reactive metabolites of HG were detected in GSH/cysteine-fortified mouse/human microsomal incubations. The cysteine conjugates were chemically synthesized for structural elucidation using manganese dioxide as the oxidizing agent. The reactive metabolites of HG were identified as quinone methide, hydroxyquinone methide, and ortho-quinone based on the fragmentation patterns of cysteine conjugates. Multiple CYP450 enzymes including CYP2D6, CYP3A4, and CYP2E1 were mediated in the formation of quinone methide, with the major role assigned to CYP2D6. While the oxidation of catechol to ortho-quinone metabolite and the subsequent isomerization into hydroxyquinone methide were independent of CYP450 isoforms. In addition, these electrophilic metabolites were found to react with biliary GSH and cysteine residues of hepatic protein in HG-treated mice. The in vitro and in vivo evidence of the metabolic activation of HG to quinone methide and ortho-quinone metabolites raised health concerns regarding the consumption of HG-containing supplements.

01 Dec 2024·Drug Testing and Analysis

Determination of higenamine in common natural spices by ultrahigh‐performance liquid chromatography–tandem mass spectrometry

Article

Author: Guo, Chengjun ; Du, Jinming ; Li, Xuefen ; Tian, Wenyi

AbstractHigenamine (HG) is a β2 receptor agonist and was explicitly added to the Prohibited List of the World Anti‐Doping Agency in 2017. This compound is prohibited in both in‐ and out‐of‐competition athletes and falls under the category of nonthreshold substances. Because of HG presence in numerous plants, as evidenced by a growing body of research data, an exception was made for HG in the TD2017MRPL document, in which adverse analytical findings (AAFs) were not reported if the urinary HG concentration was less than 10 ng/mL. In this study, a comprehensive and systematic analysis of the HG content in five batches of samples from each of the 48 natural spices selected for this investigation was conducted using UPLC–MS/MS technology. Method validation was carried out in accordance with the ICH Analytical Procedures and Methods Validation for Drugs and Biologics Guidance, and the experimental results demonstrated that the method provided appropriate sensitivity, precision, stability, linearity, and accuracy. HG was detected for the first time in Houttuynia cordata, Zingiber officinale, Cinnamomum cassia, Stevia rebaudiana, Piper nigrum, Siraitia grosuenorii, Platycodon grandiflorus, and Myristica fragrans. Furthermore, the content of HG was found to vary significantly among the different plant parts of Nelumbo nucifera, such as rhizomes, leaves, seeds, and plumules. This paper provides systematic and comprehensive data to support the safe use of spices in athletes' diets, thereby reducing the risk of food‐sourced doping violations.

100 Deals associated with Higenamine Hydrochloride

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External Link

KEGG	Wiki	ATC	Drug Bank
-	Higenamine Hydrochloride	-	DB12779

R&D Status

10 top R&D records.

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Indication	Highest Phase	Country/Location	Organization	Date
Coronary Artery Disease	Phase 3	CN	Fu Wai Hospital	10 May 2021
Coronary Artery Disease	Phase 3	CN	Institute of Materia Medica	10 May 2021
Coronary Artery Disease	Phase 3	CN	Guangdong South China New Drug Creation Center	10 May 2021
Contrast agents	Preclinical	CN	Chinese Academy of Medical Sciences	24 Aug 2012
Contrast agents	Preclinical	CN	Guangdong South China New Drug Creation Center	24 Aug 2012
Contrast agents	Preclinical	CN	Fuwai Cardiovascular Hospital	24 Aug 2012
Coronary Disease	Preclinical	CN	Guangdong South China New Drug Creation Center	24 Aug 2012
Coronary Disease	Discovery	CN	Zhuhai Rundu Pharmaceutical Co., Ltd.	24 Aug 2012
Coronary Disease	Discovery	CN	Fuwai Cardiovascular Hospital	24 Aug 2012
Coronary Disease	Discovery	CN	Chinese Academy of Medical Sciences	24 Aug 2012