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

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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152

Literatures (Medical) associated with Higenamine Hydrochloride

25 Oct 2024·ACS Sensors

Simultaneous Detection of Clenbuterol and Higenamine in Urine Samples Using Interference-Free SERS Tags Combined with Magnetic Separation

Article

Author: Liu, Dingbin ; Gao, Xia ; Sun, Chenyang ; Liu, Yaqing ; Gao, Hongmei ; Lu, Yang ; Ding, Jiacheng ; Xiao, Jinru

Sports doping remains a significant challenge in competitive sports. Given that urine analysis is the standard for detecting doping, developing rapid, sensitive, accurate, and high-throughput methods for stimulant detection in urine is crucial. Surface-enhanced Raman scattering (SERS) tag-based immunoassays have emerged as powerful analytical tools known for their high sensitivity and specificity, holding particular promise for stimulant detection in urine samples. However, both the Raman signals of typical SERS tags and sample matrices are within the Raman fingerprint region (<1800 cm^-1), which could lead to spectrum overlap, potentially reducing detection accuracy and sensitivity. By recognizing this, we designed a competitive immunoassay that integrates two types of zero-background SERS tags and magnetic separation. These innovative SERS tags exhibit distinctive Raman peaks within the Raman-silent region (1800-2800 cm^-1), effectively mitigating potential spectrum overlap with background sample signals. Moreover, magnetic separation not only enhances operational simplicity but also improves the system's anti-interference capability. Using clenbuterol (CL) and higenamine (HM) as model targets, the SERS-based competitive immunoassay demonstrated sensitive detection of individual CL or HM standards, with limits of detection (LODs) of 0.87 and 0.71 pg/mL, respectively. In multiplex mode, CL and HM can be simultaneously detected with LODs of 1.0 and 0.81 pg/mL, respectively. Furthermore, the recovery rates in urine samples ranged from 83 to 116% (relative standard deviation, RSD ≤ 6.4%) for CL and from 82 to 103% (RSD ≤ 5.1%) for HM, further confirming the reliability of the SERS-based immunoassay for practical applications.

01 Aug 2024·Journal of Pharmaceutical and Biomedical Analysis

Determination of doping higenamine in Chinese herbal medicines and their concentrated preparations by LC-MS/MS

Article

Author: Hsu, Mei-Chich ; Lin, Yi-An

The World Anti-Doping Agency (WADA) has included higenamine in the β2 agonist (S3) category of the Prohibited List since 2017 due to its pharmacological effects on adrenergic receptors. Although higenamine contained in Chinese herbal medicines has been identified by previous studies, comprehensive investigation on the higenamine content of Chinese herbs and their concentrated preparations is still required. This study aimed to determine the levels of higenamine in Chinese medicinal materials and their concentrated preparations used in Chinese medicine prescriptions in Taiwan. The levels of higenamine in Chinese medicinal materials, including Cortex Phellodendri, Flos Caryophylli, Fructus Euodiae, Fructus Kochiae, Plumula Nelumbinis, Radix Aconiti Preparata, Radix Aconiti Lateralis Preparata, and Radix Asari, and their concentrated preparations were determined by a validated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method. Our results showed that the amounts of higenamine were detected and quantified in studied Chinese medicinal materials and their concentrated preparations, except for Flos Caryophylli, Radix Aconiti Preparata, and Radix Aconiti Lateralis Preparata. Plumula Nelumbinis and Cortex Phellodendri have higher levels of higenamine when compared to other Chinese herbs tested in the present study. The highest level of higenamine was 2100 μg/g found in the Plumula Nelumbinis medicinal material. In contrast with Plumula Nelumbinis and Cortex Phellodendri, higenamine levels below 10 μg/g were found in other most of the studied Chinese medicinal materials and their concentrated preparations. This study confirmed that various Chinese herbs and their concentrated preparations contained higenamine, and it provided more coherent and comprehensive information for reducing the potential risk of higenamine misuse in sports.

01 Jun 2024·Journal of Ethnopharmacology

Mahuang Fuzi Xixin decoction alleviates allergic rhinitis by inhibiting NLRP3/Caspase-1/GSDMD-N-mediated pyroptosis

Article

Author: Tan, Xiaomei ; Wei, Xiaohan ; Liu, Changshun ; Ding, Mengze

ETHNOPHARMACOLOGICAL RELEVANCEAllergic rhinitis (AR) is a prevalent nasal inflammatory disorder, and pyroptosis plays a crucial role in aggravating AR. Current medications for AR treatment still have deficiencies, and finding new agents is of great interest. Mahuang Fuzi Xixin decoction (MFXD), an ancient Chinese medicine, is now commonly used to treat AR, which has anti-inflammatory and immunomodulatory effects, but its underlying mechanism is unknown.AIM OF THIS STUDYThis study aims to evaluate the effects of MFXD on AR and explore its potential mechanisms in view of the regulatory effect on pyroptosis.METHODSMFXD, Mahuang, Fuzi, and Xixin water extracts were analyzed using ultra high performance liquid chromatography-Orbitrap-high-resolution accurate mass spectrometry. In in vivo study, the effects of MFXD on AR treatment were evaluated in an ovalbumin-induced mouse model. Mice were administered saline (control and model groups), MFXD (1.375, 2.75 g/kg), and dexamethasone (2.5 mg/kg) for 13 days. AR symptoms were evaluated by blinded observers. Immunoglobulin E (IgE) and histamine levels were measured using enzyme-linked immunosorbent assays. Expression of pyroptosis-related proteins (NLRP3, ASC, Caspase-1 p10/p20, GSDMD-N and IL-1β) in AR mouse nasal mucosa were estimated by immunohistochemistry. In in vivtro study, the effects of MFXD on pyroptosis were assessed in human nasal epithelial cells (HNEpCs) stimulated with lipopolysaccharide (LPS) and adenosine triphosphate (ATP), and incubated with MFXD (12.5, 25, and 50 μg/mL). Pyroptosis-related protein expression was measured by western blotting.RESULTSThirty-three compounds in MFXD were identified, including ephedrine, pseudoephedrine, higenamine, aconine, aconitine, benzoylmesaconitine, benzoylhypaconine and hypaconitine. In the in vivo study, oral taken of MFXD/dexamethasone significantly ameliorated AR symptoms, reduced swelling of the nasal mucosa, and decreased the levels of IgE and histamine in AR mice serum. MFXD/dexamethasone attenuated histopathological changes and reduced the expression of pyroptosis-related proteins in nasal mucosa, indicating the inhibitory effect on nasal epithelial pyroptosis. In the in vitro study, MFXD (50 μg/mL) significantly alleviated cytotoxicity, protected cells from swelling and rupture, and downregulated the expression of pyroptosis-related proteins in LPS/ATP-induced HNEpCs.CONCLUSIONMFXD suppressed nasal epithelial pyroptosis by inhibiting the NLRP3/Caspase-1/GSDMD-N signaling pathway, which alleviates AR. Our results offer valuable insights into potential AR therapies and provide evidence for the clinical utilization of MFXD to treat AR.

100 Deals associated with Higenamine Hydrochloride

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External Link

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-	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	Guangdong South China New Drug Creation Center	10 May 2021
Coronary Artery Disease	Phase 3	CN	Zhuhai Rundu Pharmaceutical Co., Ltd.	10 May 2021
Contrast agents	Phase 2	CN	Fuwai Cardiovascular Hospital	24 Aug 2012
Contrast agents	Phase 2	CN	Guangdong South China New Drug Creation Center	24 Aug 2012
Contrast agents	Discovery	CN	Chinese Academy of Medical Sciences	24 Aug 2012
Coronary Disease	Discovery	CN	Zhuhai Rundu Pharmaceutical Co., Ltd.	24 Aug 2012
Coronary Disease	Discovery	CN	Guangdong South China New Drug Creation Center	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