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HCRTR1 Membrane Protein Introduction

Introduction of HCRTR1

Orexin receptor type 1 (Ox1R or OX1), alternatively known as HCRTR1 (Hypocretin receptor type 1), is a membrane protein which in human is encoded by HCRTR1 gene. It is recognized as a G-protein coupled receptor that is heavily expressed in projections from the lateral hypothalamus. HCRTR1 shares 64% identity with hypocretin receptor type 2 (HCRTR2), which is also called orexin receptor type 2 (Ox2R). This protein acts as a moderately selective excitatory receptor for orexin-A, and with a lower affinity for orexin-B neuropeptide.

Basic Information ofHCRTR1
Protein Name Hypocretin receptor type 1
Gene Name HCRTR1
Aliases Ox1R
Organism Homo sapiens (Human)
UniProt ID O43613
Transmembrane Times 7
Length (aa) 425
Sequence MEPSATPGAQMGVPPGSREPSPVPPDYEDEFLRYLWRDYLYPKQYEWVLIAAYVAVFVVALVGNTLVCLA
VWRNHHMRTVTNYFIVNLSLADVLVTAICLPASLLVDITESWLFGHALCKVIPYLQAVSVSVAVLTLSFI
ALDRWYAICHPLLFKSTARRARGSILGIWAVSLAIMVPQAAVMECSSVLPELANRTRLFSVCDERWADDL
YPKIYHSCFFIVTYLAPLGLMAMAYFQIFRKLWGRQIPGTTSALVRNWKRPSDQLGDLEQGLSGEPQPRA
RAFLAEVKQMRARRKTAKMLMVVLLVFALCYLPISVLNVLKRVFGMFRQASDREAVYACFTFSHWLVYAN
SAANPIIYNFLSGKFREQFKAAFSCCLPGLGPCGSLKAPSPRSSASHKSLSLQSRCSISKISEHVVLTSV
TTVLP

Function of HCRTR1 Membrane Protein

HCRTR1 selectively binds the orexin-A neuropeptide and is involved in the regulation of feeding behaviour. Normally, the activation of HCRTR1 induces cellular calcium transients in receptor-transfected cells and native receptor-expressing cells. This occurs by the increase of intracellular inositol triphosphate and subsequent release of calcium from intracellular stores. HCRTR1 is involved in multiple phospholipase activities including phospholipases C and D. HCRTR1 has also been suggested to being linked to calcium influx via the canonical transient receptor potential channel TRPC3. Other reports also demonstrated that the activation of HCRTR1 can lead to stimulation of cAMP production. Activation of HCRTR1 induces apoptosis in colon cancer cells or HCRTR1-transfected cells through Gq protein but independently of classical Gαq activation of phospholipase C and calcium pathway. Besides, a number of small-molecule HCRTR1 antagonists have been described due to their potential interest as a novel therapy for the treatment of insomnia.

Structure of HCRTR1 membrane protein. Fig.1 Structure of HCRTR1 membrane protein.

Application of HCRTR1 Membrane Protein in Literature

  1. Shahsavari F., et al. Orexin-1 receptors in the rostral ventromedial medulla are involved in the modulation of capsaicin evoked pulpal nociception and impairment of learning and memory. IntEndod J. 2018. PubMed ID: 29858522

    The results of this article suggested that rostral ventromedial medulla orexin-A receptors were involved in pulpal nociceptive modulation and improvement of learning and memory deficits induced by intradental application of capsaicin.

  2. Rezaee L., et al. Effects of intrathecal administration of orexin-1 receptor antagonist on antinociceptive responses induced by chemical stimulation of lateral hypothalamus in an animal model of tonic nociception. Neuropeptides. 2018, 69: 19-25. PubMed ID: 29735274

    This study was carried out to investigate the effects of intrathecal administration of orexin-1 receptor antagonist (SB-334867) in the spinal antinociception induced by intra-LH administration of carbachol (cholinergic receptor agonist) in both early and late phases of pain-related behaviors in the formalin test.

  3. Dong XY and Feng Z. Wake-promoting effects of vagus nerve stimulation after traumatic brain injury: upregulation of orexin-A and orexin receptor type 1 expression in the prefrontal cortex. Neural Regen Res. 2018, 13(2): 244-251. PubMed ID: 29557373

    Authors in this group indicated that vagus nerve stimulation promoted the recovery of consciousness in comatose rats after traumatic brain injury. The upregulation of orexin-A and OX1R expression in the prefrontal cortex might be involved in the wake-promoting effects of vagus nerve stimulation.

  4. Ardeshiri M.R., et al. Orexin 1 and orexin 2 receptor antagonism in the basolateral amygdala modulate long-term potentiation of the population spike in the perforant path-dentate gyrus-evoked field potential in rats. Neurobiol Learn Mem. 2018, 149: 98-106. PubMed ID: 29474954

    This article focuses on investigating the effects of orexin 1 and 2 receptor antagonism in the basolateral amygdala (BLA) on long-term potentiation (LTP) of dentate gyrus (DG) granular cells. They found that when orexin 1 and 2 receptors in the BLA were blocked after LTP induction, there were no differences between the DMSO and treatment groups.

  5. Farahimanesh S., et al. Role of orexin-1 receptors in the dorsal hippocampus (CA1 region) in expression and extinction of the morphine-induced conditioned place preference in the rats. Peptides. 2018, 101: 25-31. PubMed ID: 29269074

    Findings of this articlesupportedthatOX1rs in the CA1 region of the hippocampus were involved in the expression of morphine CPP (conditioned place preference). Moreover, blockade of OX1rs could facilitate extinction and may extinguish the ability of drug-related cues. It seemed that the antagonist might be considered as a propitious therapeutic agent in suppressing drug-seeking behaviors.

HCRTR1 Preparation Options

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