orexin-A   Click here for help

GtoPdb Ligand ID: 1697

Synonyms: hypocretin-1
Compound class: Endogenous peptide in human, mouse or rat
Comment: Additional labelled orexin-B probes that are useful experimental tools include [13C6]- and [15N]-radiolabelled peptides [2,4,13].
Species: Human, Mouse, Rat
Click here for help

Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

✖

View interactive charts of activity data across species
References
1. Ammoun S, Holmqvist T, Shariatmadari R, Oonk HB, Detheux M, Parmentier M, Akerman KE, Kukkonen JP. (2003)
Distinct recognition of OX1 and OX2 receptors by orexin peptides.
J Pharmacol Exp Ther, 305 (2): 507-14. [PMID:12606634]
2. Bårdsen K, Gjerstad MD, Partinen M, Kvivik I, Tjensvoll AB, Ruoff P, Omdal R, Brede C. (2019)
Considerably Lower Levels of Hypocretin-1 in Cerebrospinal Fluid Is Revealed by a Novel Mass Spectrometry Method Compared with Standard Radioimmunoassay.
Anal Chem, 91 (14): 9323-9329. [PMID:31260261]
3. Darker JG, Porter RA, Eggleston DS, Smart D, Brough SJ, Sabido-David C, Jerman JC. (2001)
Structure-activity analysis of truncated orexin-A analogues at the orexin-1 receptor.
Bioorg Med Chem Lett, 11 (5): 737-40. [PMID:11266181]
4. Hirtz C, Vialaret J, Gabelle A, Nowak N, Dauvilliers Y, Lehmann S. (2016)
From radioimmunoassay to mass spectrometry: a new method to quantify orexin-A (hypocretin-1) in cerebrospinal fluid.
Sci Rep, 6: 25162. [PMID:27165941]
5. Hoang QV, Bajic D, Yanagisawa M, Nakajima S, Nakajima Y. (2003)
Effects of orexin (hypocretin) on GIRK channels.
J Neurophysiol, 90 (2): 693-702. [PMID:12702704]
6. Holmqvist T, Akerman KE, Kukkonen JP. (2002)
Orexin signaling in recombinant neuron-like cells.
FEBS Lett, 526 (1-3): 11-4. [PMID:12208495]
7. Johansson L, Ekholm ME, Kukkonen JP. (2007)
Regulation of OX1 orexin/hypocretin receptor-coupling to phospholipase C by Ca2+ influx.
Br J Pharmacol, 150 (1): 97-104. [PMID:17115071]
8. Johansson L, Ekholm ME, Kukkonen JP. (2008)
Multiple phospholipase activation by OX(1) orexin/hypocretin receptors.
Cell Mol Life Sci, 65 (12): 1948-56. [PMID:18488139]
9. Jäntti M, Putula J, Somerharju P, Frohman M, Kukkonen J. (2012)
OX(1) orexin/hypocretin receptor activation of phospholipase D.
Br J Pharmacol, 165 (4b): 1109-23. [PMID:21718304]
10. Kukkonen JP. (2016)
G-protein-dependency of orexin/hypocretin receptor signalling in recombinant Chinese hamster ovary cells.
Biochem Biophys Res Commun, 476 (4): 379-85. [PMID:27237973]
11. Kukkonen JP. (2016)
OX2 orexin/hypocretin receptor signal transduction in recombinant Chinese hamster ovary cells.
Cell Signal, 28 (2): 51-60. [PMID:26582739]
12. Langmead CJ, Jerman JC, Brough SJ, Scott C, Porter RA, Herdon HJ. (2004)
Characterisation of the binding of [3H]-SB-674042, a novel nonpeptide antagonist, to the human orexin-1 receptor.
Br J Pharmacol, 141 (2): 340-6. [PMID:14691055]
13. Lindström M, Schinkelshoek M, Tienari PJ, Kukkonen JP, Renkonen R, Fronczek R, Lammers GJ, Itkonen O. (2021)
Orexin-A measurement in narcolepsy: A stability study and a comparison of LC-MS/MS and immunoassays.
Clin Biochem, 90: 34-39. [PMID:33539807]
14. Okumura T, Takeuchi S, Motomura W, Yamada H, Egashira Si S, Asahi S, Kanatani A, Ihara M, Kohgo Y. (2001)
Requirement of intact disulfide bonds in orexin-A-induced stimulation of gastric acid secretion that is mediated by OX1 receptor activation.
Biochem Biophys Res Commun, 280 (4): 976-81. [PMID:11162621]
15. Sakurai T, Amemiya A, Ishii M, Matsuzaki I, Chemelli RM, Tanaka H, Williams SC, Richardson JA, Kozlowski GP, Wilson S et al.. (1998)
Orexins and orexin receptors: a family of hypothalamic neuropeptides and G protein-coupled receptors that regulate feeding behavior.
Cell, 92 (4): 573-85. [PMID:9491897]
16. Smart D, Jerman JC, Brough SJ, Rushton SL, Murdock PR, Jewitt F, Elshourbagy NA, Ellis CE, Middlemiss DN, Brown F. (1999)
Characterization of recombinant human orexin receptor pharmacology in a Chinese hamster ovary cell-line using FLIPR.
Br J Pharmacol, 128 (1): 1-3. [PMID:10498827]
17. Tang J, Chen J, Ramanjaneya M, Punn A, Conner AC, Randeva HS. (2008)
The signalling profile of recombinant human orexin-2 receptor.
Cell Signal, 20 (9): 1651-61. [PMID:18599270]
18. Turunen PM, Ekholm ME, Somerharju P, Kukkonen JP. (2010)
Arachidonic acid release mediated by OX1 orexin receptors.
Br J Pharmacol, 159 (1): 212-21. [PMID:20002100]
19. Turunen PM, Jäntti MH, Kukkonen JP. (2012)
OX1 orexin/hypocretin receptor signaling through arachidonic acid and endocannabinoid release.
Mol Pharmacol, 82 (2): 156-67. [PMID:22550093]