Photosensitive Analogs of Epinephrine for Modulation of Biological Processes by Light

Abstract

Engineering light-sensitive molecules enables precise spatiotemporal control of biological activity using light. These molecules can be designed to respond to specific wavelengths, triggering cellular processes such as receptor activation. This strategy facilitates complex signaling studies, enhances our understanding of biological systems, and underpins the emerging field of photopharmacology with promising therapeutic potential.

Adrenergic receptors mediate the physiological effects of catecholamines like adrenaline (epinephrine) and noradrenaline (norepinephrine), regulating key functions such as heart rate, smooth muscle contraction, and metabolism. They are key targets for pharmacological agents: β-adrenergic agonists, for example, are used to treat asthma by activating β2-adrenergic receptors in airway smooth muscle to induce bronchodilation. Conversely, β-adrenergic antagonists, or beta-blockers, are employed to manage cardiovascular conditions like hypertension and arrhythmias. Agonists of α-adrenergic receptors, such as phenylephrine and oxymetazoline, are commonly used in nasal decongestants to constrict blood vessels and reduce congestion. Additionally, epinephrine is critical in treating severe allergic reactions (anaphylaxis) and is also utilized in emergencies for cardiac arrest, croup, and asthma.

Here, we present photosensitive analogs of epinephrine capable of light-triggered activation of adrenergic receptors. These compounds incorporate boron dipyrromethenes (BODIPYs) as light-harvesting antennae, conjugated to epinephrine via a carbamate linker at the meso-position. Upon green light illumination, efficient release of free epinephrine is observed. Furthermore, we demonstrate that these novel compounds modulate blood platelet activation, highlighting their potential for precise, light-controlled intervention of biological processes.
The study was supported by the Ministry of Science and Higher Education of the Russian Federation (project FSUS-2025-0011)

Speaker

Alexander Moskalensky
Novosibirsk State University
Russia

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