Target intelligence / Profile preview

Orexin Receptor 1 (OX1R)

Target
OX1R
Molecular classification
G protein-coupled receptor
01

Overview

Orexin receptor 1 (OX1R), also known as hypocretin receptor 1, is a G-protein coupled receptor (GPCR) primarily expressed in projections from the lateral hypothalamus. It plays a key role in regulating feeding behavior, arousal, wakefulness, reward processing, and locomotion. OX1R binds orexin-A with high affinity, activating phospholipase C pathways and increasing intracellular calcium.

Other names
HCRTR1Hypocretin receptor 1ORXR1OXR1
02

Mechanism of action

Gq protein activation leading to phospholipase C activation and increased intracellular calcium levels. Possible Gi protein coupling affecting cAMP levels.

03

Biological functions

Signal transductionRegulation of feeding behaviorRegulation of arousalRegulation of wakefulnessReward processingRegulation of locomotionEnergy metabolismStress responseSympathetic tone regulation
04

Disease associations

Sleep disordersAddictionMetabolic disorders
05

Safety considerations

Potential for drug interactionsDaytime somnolence
06

Interacting drugs

RTIOX-276

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