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Updated: Oct 9, 2025
08:37
Identification of Orexin and Endocannabinoid Receptors in Adult Zebrafish Using Immunoperoxidase and Immunofluorescence Methods
Published on: June 25, 2019
8.1K
Orexin receptors in GtoPdb v.2021.3.
Paul Coleman1, Luis de Lecea2, Anthony Gotter1
1Merck Research Laboratories, USA.
IUPHAR/BPS Guide to Pharmacology CITE
|December 20, 2021
Summary
Orexin receptors are activated by orexins, which are peptides derived from a common precursor. Current orexin receptor drugs, suvorexant and lemborexant, are used as hypnotics, and their crystal structures are known.
Area of Science:
- Neuroscience
- Pharmacology
Background:
- Orexin receptors are activated by endogenous peptides orexin-A and orexin-B, derived from preproorexin.
- These peptides, also known as hypocretin-1 and -2, play roles in regulating physiological functions.
- Suvorexant and lemborexant are the only orexin receptor ligands currently in clinical use as hypnotics.
Purpose of the Study:
- To provide an overview of orexin receptors, their ligands, and their clinical applications.
- To highlight the availability of orexin receptor crystal structures for further research.
Main Methods:
- Review of existing literature on orexin receptors and their ligands.
- Analysis of the nomenclature and derivation of orexins.
- Summary of current therapeutic applications and structural data.
Main Results:
- Orexin receptors are targeted by orexin-A and orexin-B.
- Suvorexant and lemborexant are established hypnotic agents acting on these receptors.
- Crystal structures of orexin receptors have been determined.
Conclusions:
- Orexin receptor research has led to the development of hypnotic drugs.
- Structural information on orexin receptors is available, facilitating drug design and understanding.
- The field continues to explore the therapeutic potential of modulating the orexin system.
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