Drug intelligence / Profile preview

higenamine

Development stage
Phase 1
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

Higenamine is a naturally occurring chemical compound found in several plants including aconite (Aconitum species), Annona squamosa (sugar apple), Nandina domestica (sacred bamboo), and others. It is structurally similar to catecholamines and acts as a stimulant with sympathomimetic properties. Higenamine functions primarily as an agonist at beta-adrenergic receptors—specifically β1 and β2 adrenoceptors—leading to increased heart rate (positive chronotropy) and enhanced cardiac contractility (positive inotropy). It also exhibits vasodilatory effects via vascular smooth muscle relaxation and bronchodilator activity through its action on β2-adrenoceptors. Additional pharmacological actions include anti-inflammatory effects via inhibition of the NF-κB signaling pathway; antioxidant activity; anti-apoptotic properties; lipid-lowering effects; antiplatelet and antithrombotic activities mediated by cAMP-dependent pathways. Higenamine has been investigated for use in cardiac stress testing and treatment of bradyarrhythmias in China but is not approved as a pharmaceutical drug or dietary supplement in most countries. It appears frequently as an undeclared ingredient in pre-workout supplements marketed for athletic performance or weight loss but is prohibited by the World Anti-Doping Agency due to its stimulant properties[1][5][6][7].

Other names
norcoclaurineO-demethylcoclaurinehigenamine hydrobromidehigenamine hydrochloridehigenamine oxalatehigenamine tartrate
02

Targets

ADRA1A (α1A)ADRB1 (β1)ADRB2 (β2)

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