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Related Experiment Video

Updated: Feb 7, 2026

Identification of Orexin and Endocannabinoid Receptors in Adult Zebrafish Using Immunoperoxidase and Immunofluorescence Methods

Identification of Orexin and Endocannabinoid Receptors in Adult Zebrafish Using Immunoperoxidase and Immunofluorescence Methods

Published on: June 25, 2019

Azulene-based compounds for targeting orexin receptors.

Teppo O Leino¹, Ainoleena Turku², Jari Yli-Kauhaluoma¹

¹Drug Research Program, Division of Pharmaceutical Chemistry and Technology, Faculty of Pharmacy, University of Helsinki, P.O. Box 56, FI-00014, University of Helsinki, Finland.

European Journal of Medicinal Chemistry

|August 6, 2018

Summary

Researchers screened 70,000 compounds, identifying novel azulene derivatives. These compounds show potential as orexin receptor antagonists, agonists, and potentiators, opening new therapeutic avenues.

Keywords:

Agonist Antagonist Azulene Orexin receptor Potentiator Sleep-wake regulation

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Published on: March 10, 2018

Area of Science:

Medicinal Chemistry
Neuropharmacology

Background:

Orexin receptors (OX1 and OX2) play crucial roles in regulating sleep-wake cycles and appetite.
Dysregulation of the orexin system is implicated in sleep disorders like narcolepsy and insomnia.

Purpose of the Study:

To discover novel small molecules targeting orexin receptors using a large-scale virtual screening approach.
To synthesize and characterize azulene-based compounds for their potential as modulators of orexin receptor activity.

Main Methods:

Virtual screening of a 70,000-compound library of synthetically accessible azulene derivatives against the OX2 receptor.
Synthesis of selected azulene derivatives.
In vitro assessment of binding affinity and functional activity (agonism/antagonism/potentiation) at both OX1 and OX2 receptors.

Main Results:

Two azulene derivatives demonstrated significant binding to orexin receptors with inhibition constants in the micromolar range.
Two compounds exhibited weak agonistic activity at the OX2 receptor.
Three compounds showed concentration-dependent potentiation of orexin-A response at the OX1 receptor, but not OX2.

Conclusions:

The azulene scaffold is a promising starting point for developing novel modulators of the orexin system.
Identified compounds provide a foundation for further optimization into potential therapeutic agents for orexin-related disorders.
This study highlights the utility of virtual screening in identifying novel chemical matter for complex biological targets.