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Target intelligence / Profile preview
Orexin Receptor (ORX-R)
- Target
- ORX-R
- Molecular classification
- G protein-coupled receptor, GPCR, Receptor
01
Overview
The orexin receptor is a G-protein-coupled receptor that binds the neuropeptides orexin-A and orexin-B. There are two main subtypes: OX1R (HCRTR1) and OX2R (HCRTR2). These receptors play crucial roles in regulating sleep-wake cycles, feeding behavior, and reward-seeking behavior. Antagonists targeting these receptors are used for treating sleep disorders like insomnia. Orexin receptors couple primarily to Gq/11 proteins, activating downstream effectors such as phospholipase C (PLC), leading to inositol trisphosphate (IP₃) production and increased intracellular Ca²⁺ levels.
- Other names
- Hypocretin receptor
02
Mechanism of action
Antagonism of orexin receptors, leading to decreased wakefulness.
03
Biological functions
Sleep-wake regulationFeeding behaviorAppetite controlReward-seeking behaviorAddictionLocomotionSympathetic toneEnergy homeostasisNeuroexcitationSignal transductionModulation of synaptic plasticityCalcium signaling
04
Disease associations
Sleep disordersInsomniaNarcolepsyAddiction
05
Interacting drugs
Suvorexant
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