Page last updated: 2024-11-13

orexin-a

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID56842143
MeSH IDM0287275

Synonyms (10)

Synonym
205599-75-3
orexin a
orexin-a
orexine a
unii-8rdy08v4vc
8rdy08v4vc ,
oroxin-a
HB2937
xplpdccrqktcscrlyellhgagnhaagiltl (modifications: c-terminal amide; x-1 = glp; disulfide bonds: 6-12, 7-14)
c152h243n47o44s4
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (3)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Orexin receptor type 1Homo sapiens (human)Ki0.01290.00030.28763.1623AID150548
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Orexin receptor type 1Homo sapiens (human)EC50 (µMol)0.01010.00010.50622.5000AID1062207; AID1878169; AID767535
Orexin receptor type 2Homo sapiens (human)EC50 (µMol)0.01310.00010.01990.0600AID1062205; AID1878172; AID767534
Cytochrome P450 1A2Homo sapiens (human)EC50 (µMol)0.00110.00030.20692.0000AID1062205
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (34)

Processvia Protein(s)Taxonomy
neuropeptide signaling pathwayOrexin receptor type 1Homo sapiens (human)
chemical synaptic transmissionOrexin receptor type 1Homo sapiens (human)
feeding behaviorOrexin receptor type 1Homo sapiens (human)
regulation of cytosolic calcium ion concentrationOrexin receptor type 1Homo sapiens (human)
positive regulation of ERK1 and ERK2 cascadeOrexin receptor type 1Homo sapiens (human)
cellular response to hormone stimulusOrexin receptor type 1Homo sapiens (human)
phospholipase C-activating G protein-coupled receptor signaling pathwayOrexin receptor type 2Homo sapiens (human)
neuropeptide signaling pathwayOrexin receptor type 2Homo sapiens (human)
chemical synaptic transmissionOrexin receptor type 2Homo sapiens (human)
feeding behaviorOrexin receptor type 2Homo sapiens (human)
regulation of circadian sleep/wake cycle, wakefulnessOrexin receptor type 2Homo sapiens (human)
circadian sleep/wake cycle processOrexin receptor type 2Homo sapiens (human)
locomotionOrexin receptor type 2Homo sapiens (human)
regulation of cytosolic calcium ion concentrationOrexin receptor type 2Homo sapiens (human)
cellular response to hormone stimulusOrexin receptor type 2Homo sapiens (human)
steroid catabolic processCytochrome P450 1A2Homo sapiens (human)
porphyrin-containing compound metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 1A2Homo sapiens (human)
cholesterol metabolic processCytochrome P450 1A2Homo sapiens (human)
estrogen metabolic processCytochrome P450 1A2Homo sapiens (human)
toxin biosynthetic processCytochrome P450 1A2Homo sapiens (human)
post-embryonic developmentCytochrome P450 1A2Homo sapiens (human)
alkaloid metabolic processCytochrome P450 1A2Homo sapiens (human)
regulation of gene expressionCytochrome P450 1A2Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 1A2Homo sapiens (human)
dibenzo-p-dioxin metabolic processCytochrome P450 1A2Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
lung developmentCytochrome P450 1A2Homo sapiens (human)
methylationCytochrome P450 1A2Homo sapiens (human)
monocarboxylic acid metabolic processCytochrome P450 1A2Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 1A2Homo sapiens (human)
retinol metabolic processCytochrome P450 1A2Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 1A2Homo sapiens (human)
cellular respirationCytochrome P450 1A2Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 1A2Homo sapiens (human)
hydrogen peroxide biosynthetic processCytochrome P450 1A2Homo sapiens (human)
oxidative demethylationCytochrome P450 1A2Homo sapiens (human)
cellular response to cadmium ionCytochrome P450 1A2Homo sapiens (human)
omega-hydroxylase P450 pathwayCytochrome P450 1A2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (19)

Processvia Protein(s)Taxonomy
G protein-coupled receptor activityOrexin receptor type 1Homo sapiens (human)
protein bindingOrexin receptor type 1Homo sapiens (human)
orexin receptor activityOrexin receptor type 1Homo sapiens (human)
peptide hormone bindingOrexin receptor type 1Homo sapiens (human)
peptide bindingOrexin receptor type 1Homo sapiens (human)
protein bindingOrexin receptor type 2Homo sapiens (human)
neuropeptide receptor activityOrexin receptor type 2Homo sapiens (human)
orexin receptor activityOrexin receptor type 2Homo sapiens (human)
peptide hormone bindingOrexin receptor type 2Homo sapiens (human)
peptide bindingOrexin receptor type 2Homo sapiens (human)
monooxygenase activityCytochrome P450 1A2Homo sapiens (human)
iron ion bindingCytochrome P450 1A2Homo sapiens (human)
protein bindingCytochrome P450 1A2Homo sapiens (human)
electron transfer activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activityCytochrome P450 1A2Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 1A2Homo sapiens (human)
enzyme bindingCytochrome P450 1A2Homo sapiens (human)
heme bindingCytochrome P450 1A2Homo sapiens (human)
demethylase activityCytochrome P450 1A2Homo sapiens (human)
caffeine oxidase activityCytochrome P450 1A2Homo sapiens (human)
aromatase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 1A2Homo sapiens (human)
hydroperoxy icosatetraenoate dehydratase activityCytochrome P450 1A2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (4)

Processvia Protein(s)Taxonomy
plasma membraneOrexin receptor type 1Homo sapiens (human)
synapseOrexin receptor type 1Homo sapiens (human)
plasma membraneOrexin receptor type 1Homo sapiens (human)
plasma membraneOrexin receptor type 2Homo sapiens (human)
synapseOrexin receptor type 2Homo sapiens (human)
plasma membraneOrexin receptor type 2Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 1A2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

Assay IDTitleYearJournalArticle
AID51935Functional potency was determined by concentration required for activation of OX1 (Orexin-1) receptor expressed in chinese hamster ovary cells (CHO) and increasing the intracellular calcium concentration2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.
AID767534Agonist activity at OX2 receptor (unknown origin) expressed in RD-HGA16 cells assessed as calcium mobilization by fluorescence assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.
AID1062205Agonist activity at human OX2 receptor overexpressed in CHO-RD-HGA16 cells assessed as calcium mobilization after 15 mins by fluorescence assay2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
Truncated Orexin Peptides: Structure-Activity Relationship Studies.
AID1062207Agonist activity at human OX1 receptor overexpressed in CHO-RD-HGA16 cells assessed as calcium mobilization after 15 mins by fluorescence assay2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
Truncated Orexin Peptides: Structure-Activity Relationship Studies.
AID767535Agonist activity at OX1 receptor (unknown origin) expressed in RD-HGA16 cells assessed as calcium mobilization by fluorescence assay2013Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.
AID1062203Selectivity ratio of EC50 for human OX2 receptor to EC50 for human OX1 receptor2013ACS medicinal chemistry letters, Dec-12, Volume: 4, Issue:12
Truncated Orexin Peptides: Structure-Activity Relationship Studies.
AID1878175Selectivity index, ratio of EC50 for agonist activity at OX1R (unknown origin) to EC50 for agonist activity at OX2R (unknown origin)
AID1878169Agonist activity at OX1R (unknown origin)
AID150548Binding affinity to Orexin receptor type 1 was determined using laser scanning cytometry2001Bioorganic & medicinal chemistry letters, Mar-12, Volume: 11, Issue:5
Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.
AID1249695Induction of wakefullness in C57BL/6J mouse assessed as increase in wake time by measuring EEG/EMG signals at 3 nmol, icv dosed on every other day during light phase2015Journal of medicinal chemistry, Oct-22, Volume: 58, Issue:20
Design and Synthesis of Non-Peptide, Selective Orexin Receptor 2 Agonists.
AID1878172Agonist activity at OX2R (unknown origin)
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (5)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's1 (20.00)29.6817
2010's3 (60.00)24.3611
2020's1 (20.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 57.96

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index57.96 (24.57)
Research Supply Index1.79 (2.92)
Research Growth Index4.92 (4.65)
Search Engine Demand Index87.62 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (57.96)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]