Related Experiment Video

Updated: Oct 22, 2025

Polygraphic Recording Procedure for Measuring Sleep in Mice
08:45

Polygraphic Recording Procedure for Measuring Sleep in Mice

Published on: January 25, 2016

24.5K

Orexin receptors: Targets and applications

Subhiksha Subramanian1, Mirunalini Ravichandran1

  • 1Department of Pharmacology, Jawaharlal Institute of Postgraduate Medical Education and Research, Puducherry, India.

Fundamental & Clinical Pharmacology
|August 31, 2021
PubMed

Insights

Orexins, hypothalamic neuropeptides, target G-protein coupled receptors (GPCRs) for treating neurological and other disorders. This review details orexin receptor structure, function, and therapeutic applications, including recent drug approvals.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Endocrinology

Background:

  • Orexins are hypothalamic neuropeptides regulating physiological and pathological processes.
  • G-protein coupled receptors (GPCRs) are key drug targets for numerous diseases.
  • Orexin receptors have evolved from orphan receptors to significant therapeutic targets.

Purpose of the Study:

  • To provide a comprehensive review of orexin receptors.
  • To discuss their structure, physiological roles, and therapeutic applications.
  • To summarize recent advancements in orexin receptor-targeted drug discovery.

Main Methods:

  • Literature review of orexin receptor research.
  • Analysis of orexin receptor structure and function.
  • Examination of therapeutic applications and drug development.

Main Results:

  • Orexin receptors play crucial roles in various physiological functions.
  • Dysregulation of orexin signaling is implicated in disorders like insomnia and obesity.
  • Orexin receptor antagonists and agonists show therapeutic potential.

Conclusions:

  • Orexin receptors are promising targets for treating a range of disorders.
  • Further research into orexin receptor pharmacology can yield novel therapeutics.
  • Recent drug approvals highlight the clinical significance of targeting the orexin system.
Keywords:
agonistantagonistorexin systemphysiological role

More Related Videos

Author Spotlight: Hypothalamic Neural Mechanism Insights09:29

Author Spotlight: Hypothalamic Neural Mechanism Insights

Published on: August 4, 2023

4.1K
Optogenetic Manipulation of Neural Circuits During Monitoring Sleep/wakefulness States in Mice08:58

Optogenetic Manipulation of Neural Circuits During Monitoring Sleep/wakefulness States in Mice

Published on: June 19, 2019

10.0K

Related Concept Videos

Opioid Receptors: Overview01:22

Opioid Receptors: Overview

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,...
2.5K
G Protein-coupled Receptors01:15

G Protein-coupled Receptors

G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
14.1K
Sleep-Wake Cycles01:24

Sleep-Wake Cycles

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:
1.9K
Sedatives and Hypnotics Drugs: Miscellaneous Agents01:17

Sedatives and Hypnotics Drugs: Miscellaneous Agents

Sedatives and hypnotics encompass a wide range of substances, each with its unique mechanism of action, uses, and potential adverse effects.
Melatonin congeners like ramelteon (Rozerem) and tasimelteon (Hetlioz) selectively bind to melatonin receptors (MT1 and MT2) and thus mimic the actions of melatonin, a hormone that regulates sleep-wake cycles. Tasimelteon is primarily used for non-24-hour sleep-wake disorder, common in blind patients. They are also used to treat conditions like insomnia...
286
Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:
1.9K
Transducer Mechanism: G Protein–Coupled Receptors01:30

Transducer Mechanism: G Protein–Coupled Receptors

G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
GPCRs are also called heptahelical,...
2.9K