Page last updated: 2024-08-07 12:43:58

Orexin receptor type 1

An orexin/hypocretin receptor type 1 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O43613]

Synonyms

Ox-1-R;
Ox1-R;
Ox1R;
Hypocretin receptor type 1

Research

Bioassay Publications (29)

TimeframeStudies on this Protein(%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's5 (17.24)29.6817
2010's20 (68.97)24.3611
2020's4 (13.79)2.80

Compounds (16)

Drugs with Inhibition Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
sb 408124Homo sapiens (human)Ki0.023622
sb 334867-aHomo sapiens (human)IC509.020022
sb 334867-aHomo sapiens (human)Ki0.024044
nalfurafine hydrochlorideHomo sapiens (human)Ki0.250011
jnj 10397049Homo sapiens (human)Ki1.864555
sb674042Homo sapiens (human)Ki0.002522
tcs ox2 29Homo sapiens (human)IC5010.000033
almorexantHomo sapiens (human)IC500.039544
almorexantHomo sapiens (human)Ki0.013011
suvorexantHomo sapiens (human)IC500.087244
suvorexantHomo sapiens (human)Ki0.001066
mk-6096Homo sapiens (human)IC500.013522
mk-6096Homo sapiens (human)Ki0.002155
sb 649868Homo sapiens (human)Ki0.000444
act-462206Homo sapiens (human)IC500.060022
act-462206Homo sapiens (human)Ki0.006311
gsk 1059865Homo sapiens (human)Ki0.002011
act-335827Homo sapiens (human)IC500.006033
act-335827Homo sapiens (human)Ki0.006011
orexin-aHomo sapiens (human)Ki0.012911

Drugs with Activation Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
sb 408124Homo sapiens (human)Kd0.026911
sb674042Homo sapiens (human)Kd0.005111
oroxin bHomo sapiens (human)EC501.250422
orexin-aHomo sapiens (human)EC500.010133

Drugs with Other Measurements

DrugTaxonomyMeasurementAverage (mM)Bioassay(s)Publication(s)
sr141716Homo sapiens (human)Ke6.667033
sb 334867-aHomo sapiens (human)Ke0.045011
gsk 1059865Homo sapiens (human)Kb0.001611

Enables

This protein enables 5 target(s):

TargetCategoryDefinition
G protein-coupled receptor activitymolecular functionCombining with an extracellular signal and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:bf, http://www.iuphar-db.org, Wikipedia:GPCR]
protein bindingmolecular functionBinding to a protein. [GOC:go_curators]
orexin receptor activitymolecular functionCombining with orexin to initiate a change in cell activity. [GOC:ai]
peptide hormone bindingmolecular functionBinding to a peptide with hormonal activity in animals. [GOC:jl, ISBN:0198506732]
peptide bindingmolecular functionBinding to a peptide, an organic compound comprising two or more amino acids linked by peptide bonds. [GOC:jl]

Located In

This protein is located in 2 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]
synapsecellular componentThe junction between an axon of one neuron and a dendrite of another neuron, a muscle fiber or a glial cell. As the axon approaches the synapse it enlarges into a specialized structure, the presynaptic terminal bouton, which contains mitochondria and synaptic vesicles. At the tip of the terminal bouton is the presynaptic membrane; facing it, and separated from it by a minute cleft (the synaptic cleft) is a specialized area of membrane on the receiving cell, known as the postsynaptic membrane. In response to the arrival of nerve impulses, the presynaptic terminal bouton secretes molecules of neurotransmitters into the synaptic cleft. These diffuse across the cleft and transmit the signal to the postsynaptic membrane. [GOC:aruk, ISBN:0198506732, PMID:24619342, PMID:29383328, PMID:31998110]

Active In

This protein is active in 1 target(s):

TargetCategoryDefinition
plasma membranecellular componentThe membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363]

Involved In

This protein is involved in 6 target(s):

TargetCategoryDefinition
neuropeptide signaling pathwaybiological processA G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194]
chemical synaptic transmissionbiological processThe vesicular release of classical neurotransmitter molecules from a presynapse, across a chemical synapse, the subsequent activation of neurotransmitter receptors at the postsynapse of a target cell (neuron, muscle, or secretory cell) and the effects of this activation on the postsynaptic membrane potential and ionic composition of the postsynaptic cytosol. This process encompasses both spontaneous and evoked release of neurotransmitter and all parts of synaptic vesicle exocytosis. Evoked transmission starts with the arrival of an action potential at the presynapse. [GOC:jl, MeSH:D009435]
feeding behaviorbiological processBehavior associated with the intake of food. [GOC:mah]
regulation of cytosolic calcium ion concentrationbiological processAny process involved in the maintenance of an internal steady state of calcium ions within the cytosol of a cell or between the cytosol and its surroundings. [GOC:ai, GOC:mah, GOC:rph]
positive regulation of ERK1 and ERK2 cascadebiological processAny process that activates or increases the frequency, rate or extent of signal transduction mediated by the ERK1 and ERK2 cascade. [GOC:mah]
cellular response to hormone stimulusbiological processAny process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a hormone stimulus. [GOC:mah]