Target intelligence / Profile preview

Orexin/Hypocretin Receptor Type 2 (OX2R)

Target
OX2R
Molecular classification
G-protein coupled receptor (GPCR), GPCR 1 family
01

Overview

Orexin/Hypocretin Receptor Type 2 (OX2R) is a G-protein coupled receptor that binds orexin-A and orexin-B. It is primarily expressed in the brain, particularly in wake-promoting regions. OX2R plays a critical role in sleep-wake regulation, feeding behavior, energy homeostasis, reward, and neuroendocrine functions. Disruptions in OX2R signaling are linked to sleep disorders like narcolepsy, and it is a therapeutic target for insomnia, with dual orexin receptor antagonists like suvorexant used in treatment. Selective antagonists are under investigation to improve the therapeutic profile. OX2R is also implicated in neurological diseases such as depression, Alzheimer’s disease, ischemic stroke, and drug addiction.

Other names
Ox-2-ROx2-RHypocretin receptor type 2HCRTR2
02

Mechanism of action

Dual orexin receptor antagonist; blocking both OX1R and OX2R.

03

Biological functions

Sleep-wake regulationFeeding behaviorEnergy homeostasisReward & addictionNeuroendocrine & stress responseSignal transduction
04

Disease associations

Sleep disordersNarcolepsyDepressionAlzheimer’s diseaseIschemic strokeDrug addiction
05

Safety considerations

Potential side effects associated with dual orexin receptor antagonism.Therapeutic challenges in selectively targeting OX₂ receptors.
06

Interacting drugs

Suvorexant

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