Related Experiment Video
Updated: Feb 28, 2026

08:45
Polygraphic Recording Procedure for Measuring Sleep in Mice
Published on: January 25, 2016
25.5K
Orexin research: patent news from 2016
Christoph Boss1, Catherine Roch1
1a Drug Discovery and Preclinical Research , Actelion Pharmaceuticals Ltd , Allschwil , Switzerland.
Expert Opinion on Therapeutic Patents
|June 21, 2017
Summary
The orexin system, crucial for wakefulness and implicated in anxiety and addiction, is a key target for new insomnia and narcolepsy treatments. Research focuses on orexin receptor agonists and antagonists for therapeutic development.
Area of Science:
- Neuroscience
- Pharmacology
- Drug Discovery
Background:
- The orexin system, comprising two receptors (orexin 1 and 2) and two ligands (orexin A and B), regulates wakefulness, anxiety, and addiction.
- Orexin receptor activation can induce apoptosis in cancer cells, and dual orexin receptor antagonists are approved for insomnia.
- Clinical validation of selective orexin 1 receptor antagonists and the potential of orexin agonism for narcolepsy with cataplexy are key research areas.
Purpose of the Study:
- To review patent applications related to orexin receptors filed in 2016.
- To discuss recent scientific findings concerning orexin receptor targets.
- To provide expert opinion on the current state and future directions of orexin receptor research.
Main Methods:
- Literature review of scientific publications.
- Analysis of patent applications from the Thomson Reuters Integrity Database (2016).
- Synthesis of existing data and expert commentary.
Main Results:
- A significant number of patents indicate sustained interest in orexin receptors as therapeutic targets.
- The structural diversity in patented compounds is limited, raising questions about novelty.
- New X-ray structure data for orexin receptors may facilitate the optimization of antagonists and the discovery of agonists.
Conclusions:
- Orexin receptor antagonists show promise for insomnia, while agonists are being explored for narcolepsy with cataplexy.
- Continued research, aided by structural biology, is essential for developing novel orexin-targeting therapeutics.
- The field is dynamic, with ongoing efforts to validate orexin receptor modulators for various neurological and psychiatric conditions.
Related Concept Videos
Circadian Rhythms and Gene Regulation
4.6K
The biological clock is involved in many aspects of regulating complex physiology in all animals. It was in 1935 when German zoologists, Hans Kalmus and Erwin Bünning, discovered the existence of circadian rhythm in Drosophila melanogaster. However, the internal molecular mechanisms behind the circadian clock remained a mystery until 1984, when Jeffrey C. Hall, Michael Rosbash, and Michael W. Young discovered the expression of the Per gene oscillating over a 24-hour cycle. In subsequent...
4.6K
Sleep-Wake Cycles
3.1K
Sleep is an essential physiological process vital to maintaining overall well-being. The reticular activating system (RAS), a network of neurons in the brainstem, regulates wakefulness and sleep. While it may seem passive, sleep consists of distinct cycles, each with its unique characteristics and functions. Two key sleep phases are non-rapid eye movement (NREM) and rapid eye movement (REM).
NREM Sleep
NREM sleep comprises four progressive stages that seamlessly merge:
NREM Sleep
NREM sleep comprises four progressive stages that seamlessly merge:
3.1K
Channel Rhodopsins
3.3K
Most organisms use photoreceptors to sense and respond to light. Examples of photoreceptors include bacteriorhodopsins and bacteriophytochromes in some bacteria, phytochromes in plants, and rhodopsins in the photoreceptor cells of the vertebral retina. The light-sensitive property of these receptors is because of the bound chromophores, such as bilin in the phytochromes and retinal in the rhodopsins.
Rhodopsins belong to the family of cell surface proteins called G-protein coupled receptors,...
Rhodopsins belong to the family of cell surface proteins called G-protein coupled receptors,...
3.3K
Drug Regulation
3.2K
Drug regulation encompasses the management of drug usage by evaluating its safety and efficacy through assessments conducted by regulatory authorities. Regrettably, the history of drug regulation is marred by several catastrophic events. One such incident is the Elixir Sulfanilamide tragedy, in which the toxic compound diethyl glycol was included in a sweet-tasting medication, leading to numerous fatalities. This event prompted the enactment of the Food, Drug, and Cosmetic Act in 1938. Under...
3.2K
Opioid Receptors: Overview
5.4K
Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2,...
5.4K
Regulation of the Unfolded Protein Response
3.1K
Inositol-requiring kinase one or IRE1 is the most conserved eukaryotic unfolded protein response (UPR) receptor. It is a type I transmembrane protein kinase receptor with a distinctive site-specific RNase activity. As the binding mechanics of the misfolded proteins with the N-terminal domain of IRE-1 are unclear, three binding models — direct, indirect, and allosteric -- are proposed for receptor activation. Nevertheless, it is known that once a misfolded protein associates with IRE1, it...
3.1K

