Higenamine
STIMULANTAlso known as: Norcoclaurine, Demethylcoclaurine, 1-[(4-hydroxyphenyl)methyl]-1,2,3,4-tetrahydroisoquinoline-6,7-diol
What is Higenamine?
Higenamine is a β2-adrenergic agonist found naturally in lotus seeds, Nandina domestica, aconite root, and beetroot. FDA determined it requires New Dietary Ingredient notification (none submitted). WADA banned since 2017—has ended athletic careers including UEFA footballer Mamadou Sakho.
Why is Higenamine Banned?
New Dietary Ingredient without required FDA premarket notification. WADA prohibited as β2-agonist at all times. Career-ending for competitive athletes in any sport.
Health Risks & Side Effects
Health Risk Level
This substance has a moderate risk of overdose and low addiction potential.
warningCommon Side Effects
- arrow_rightTachycardia
- arrow_rightPalpitations
- arrow_rightTremor
- arrow_rightAnxiety
- arrow_rightHeadache
- arrow_rightArrhythmias
blockContraindications
- arrow_rightCompetitive athletes (career-ending)
- arrow_rightHeart conditions
- arrow_rightArrhythmias
- arrow_rightAsthma medication use (β2 agonists)
How Does Higenamine Work?
Activates β2-adrenergic receptors causing bronchodilation, increased heart rate, and thermogenesis. Effects similar to ephedrine and other banned β2 agonists.
History
Traditional use in Chinese medicine (lotus seeds). Emerged in pre-workout supplements around 2015. WADA added to prohibited list effective January 2017. FDA issued warning letters May 2022 for missing NDI notifications.
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Research articles and educational resources
Overview
Higenamine
Higenamine (norcoclaurine) is a chemical compound found in a variety of plants including Nandina domestica (fruit), Aconitum carmichaelii (root), Asarum heterotropioides, Galium divaricatum, Annona squamosa, and Nelumbo nucifera.
Scientific Research
From PubMed • 3 peer-reviewed studies
Applications of Higenamine in pharmacology and medicine.
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.
Higenamine as a Potential Pharmacologic Stress Agent in the Detection of Coronary Artery Disease.
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.
Unauthorized ingredients in "nootropic" dietary supplements: A review of the history, pharmacology, prevalence, international regulations, and potential as doping agents.
The first nootropic prohibited in sport was fonturacetam (4-phenylpiracetam, carphedon) in 1998. Presented here 25 years later is a broad-scale consideration of the history, pharmacology, prevalence, regulations, and doping potential of nootropics viewed through a lens of 50 selected dietary supplements (DS) marketed as "cognitive enhancement," "brain health," "brain boosters," or "nootropics," with a focus on unauthorized ingredients. Nootropic DS have risen to prominence over the last decade often as multicomponent formulations of bioactive ingredients presenting compelling pharmacological questions and potential public health concerns. Many popular nootropics are unauthorized food or DS ingredients according to the European Commission including huperzine A, yohimbine, and dimethylaminoethanol; unapproved pharmaceuticals like phenibut or emoxypine (mexidol); previously registered drugs like meclofenoxate or reserpine; EU authorized pharmaceuticals like piracetam or vinpocetine; infamous doping agents like methylhexaneamine or dimethylbutylamine; and other investigational substances and peptides. Several are authorized DS ingredients in the United States resulting in significant global variability as to what qualifies as a legal nootropic. Prohibited stimulants or ß2-agonists commonly used in "pre-workout," "weight loss," or "thermogenic" DS such as octodrine, hordenine, or higenamine are often stacked with nootropic substances. While stimulants and ß2-agonists are defined as doping agents by the World Anti-Doping Agency (WADA), many nootropics are not, although some may qualify as non-approved substances or related substances under catch-all language in the WADA Prohibited List. Synergistic combinations, excessive dosing, or recently researched pharmacology may justify listing certain nootropics as doping agents or warrant additional attention in future regulations.