Page last updated: 2024-08-07 15:25:37
Orexin receptor type 2
An orexin receptor type 2 that is encoded in the genome of human. [PRO:DNx, UniProtKB:O43614]
Synonyms
Ox-2-R;
Ox2-R;
Ox2R;
Hypocretin receptor type 2
Research
Bioassay Publications (25)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (16.00) | 29.6817 |
| 2010's | 18 (72.00) | 24.3611 |
| 2020's | 3 (12.00) | 2.80 |
Compounds (14)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| oroxin b | Homo sapiens (human) | EC50 | 0.0300 | 2 | 2 |
| orexin-a | Homo sapiens (human) | EC50 | 0.0131 | 3 | 3 |
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| sb 334867-a | Homo sapiens (human) | Ke | 1.1940 | 1 | 1 |
| gsk 1059865 | Homo sapiens (human) | Kb | 0.1260 | 1 | 1 |
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases.European journal of medicinal chemistry, , Nov-01, Volume: 181, 2019
Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Diaryl urea analogues of SB-334867 as orexin-1 receptor antagonists.Bioorganic & medicinal chemistry letters, , May-15, Volume: 21, Issue:10, 2011
Novel Octahydropyrrolo[3,4-c]pyrroles Are Selective Orexin-2 Antagonists: SAR Leading to a Clinical Candidate.Journal of medicinal chemistry, , Jul-23, Volume: 58, Issue:14, 2015
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Novel substituted 4-phenyl-[1,3]dioxanes: potent and selective orexin receptor 2 (OX(2)R) antagonists.Bioorganic & medicinal chemistry letters, , Aug-16, Volume: 14, Issue:16, 2004
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
N-acyl 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline: the first orexin-2 receptor selective non-peptidic antagonist.Bioorganic & medicinal chemistry letters, , Dec-15, Volume: 13, Issue:24, 2003
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 23, Issue:13, 2013
Biomedical application of orexin/hypocretin receptor ligands in neuroscience.Journal of medicinal chemistry, , Feb-26, Volume: 52, Issue:4, 2009
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Discovery of novel substituted octahydropyrrolo[3,4-c]pyrroles as dual orexin receptor antagonists for insomnia treatment.Bioorganic & medicinal chemistry letters, , 03-15, Volume: 27, Issue:6, 2017
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Discovery of diazepane amide DORAs and 2-SORAs enabled by exploration of isosteric quinazoline replacements.Bioorganic & medicinal chemistry letters, , Nov-01, Volume: 25, Issue:21, 2015
Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis.Bioorganic & medicinal chemistry letters, , May-01, Volume: 24, Issue:9, 2014
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Discovery of the dual orexin receptor antagonist [(7R)-4-(5-chloro-1,3-benzoxazol-2-yl)-7-methyl-1,4-diazepan-1-yl][5-methyl-2-(2H-1,2,3-triazol-2-yl)phenyl]methanone (MK-4305) for the treatment of insomnia.Journal of medicinal chemistry, , Jul-22, Volume: 53, Issue:14, 2010
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Recent trends in orexin research--2010 to 2015.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
Discovery of piperidine ethers as selective orexin receptor antagonists (SORAs) inspired by filorexant.Bioorganic & medicinal chemistry letters, , Feb-01, Volume: 25, Issue:3, 2015
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Design, synthesis, and structure-activity relationships of a series of novel N-aryl-2-phenylcyclopropanecarboxamide that are potent and orally active orexin receptor antagonists.Bioorganic & medicinal chemistry, , Nov-01, Volume: 22, Issue:21, 2014
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Discovery process and pharmacological characterization of a novel dual orexin 1 and orexin 2 receptor antagonist useful for treatment of sleep disorders.Bioorganic & medicinal chemistry letters, , Sep-15, Volume: 21, Issue:18, 2011
2-Methyl-3-furanyl-4H-1,2,4-triazol-3-ylthioamides: a new class of selective orexin 2 antagonists.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 20, Issue:22, 2010
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Orexin Receptor Antagonists: New Therapeutic Agents for the Treatment of Insomnia.Journal of medicinal chemistry, , Jan-28, Volume: 59, Issue:2, 2016
Recent trends in orexin research--2010 to 2015.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
[no title available]Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.Bioorganic & medicinal chemistry letters, , Jan-06, Volume: 13, Issue:1, 2003
Comparison of Orexin 1 and Orexin 2 Ligand Binding Modes Using X-ray Crystallography and Computational Analysis.Journal of medicinal chemistry, , 02-27, Volume: 63, Issue:4, 2020
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
Substituted Azabicyclo[2.2.1]heptanes as Selective Orexin-1 Antagonists: Discovery of JNJ-54717793.ACS medicinal chemistry letters, , Oct-08, Volume: 11, Issue:10, 2020
Discovery of highly potent and selective orexin 1 receptor antagonists (1-SORAs) suitable for in vivo interrogation of orexin 1 receptor pharmacology.Bioorganic & medicinal chemistry letters, , 12-01, Volume: 26, Issue:23, 2016
Recent trends in orexin research--2010 to 2015.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 25, Issue:15, 2015
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Selective orexin receptor antagonists.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 23, Issue:17, 2013
[no title available]Bioorganic & medicinal chemistry letters, , 03-15, Volume: 60, 2022
Substituted tetrahydroisoquinolines as selective antagonists for the orexin 1 receptor.Journal of medicinal chemistry, , Sep-12, Volume: 56, Issue:17, 2013
Truncated Orexin Peptides: Structure-Activity Relationship Studies.ACS medicinal chemistry letters, , Dec-12, Volume: 4, Issue:12, 2013
Enables
This protein enables 5 target(s):
| Target | Category | Definition |
|---|
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| neuropeptide receptor activity | molecular function | Combining with a neuropeptide to initiate a change in cell activity. [GOC:ai] |
| orexin receptor activity | molecular function | Combining with orexin to initiate a change in cell activity. [GOC:ai] |
| peptide hormone binding | molecular function | Binding to a peptide with hormonal activity in animals. [GOC:jl, ISBN:0198506732] |
| peptide binding | molecular function | Binding 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):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| synapse | cellular component | The 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):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The 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 9 target(s):
| Target | Category | Definition |
|---|
| phospholipase C-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of phospholipase C (PLC) and a subsequent increase in the intracellular concentration of inositol trisphosphate (IP3) and diacylglycerol (DAG). [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |
| neuropeptide signaling pathway | biological process | A 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 transmission | biological process | The 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 behavior | biological process | Behavior associated with the intake of food. [GOC:mah] |
| regulation of circadian sleep/wake cycle, wakefulness | biological process | Any process that modulates the rate, frequency, or extent of the wakeful phase of the circadian sleep/wake cycle. The wakeful phase is the part of the circadian sleep/wake cycle where the organism is not asleep. [GOC:dph, GOC:tb] |
| circadian sleep/wake cycle process | biological process | A behavioral process involved in the cycle from wakefulness through an orderly succession of sleep states and stages that occurs on an approximately 24 hour rhythm. [GOC:isa_complete] |
| locomotion | biological process | Self-propelled movement of a cell or organism from one location to another. [GOC:dgh] |
| regulation of cytosolic calcium ion concentration | biological process | Any 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] |
| cellular response to hormone stimulus | biological process | Any 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] |