[Ala11, D-Leu15]orexin-B   Click here for help

GtoPdb Ligand ID: 1700

Compound class: Peptide or derivative
Comment: Synthetic analogue of human orexin-B [1]. Reduced potency as compared to orexin-B but more reduced at OX1 giving higher selectivity for OX2 than orexin-B [1-2]. Very different selectivities have been reported: 15-fold selective for OX2 in Chinese hamster ovary (CHO-K1) cells and 23-fold selective in human embryonic kidney (HEK293) cells (the selectivity of orexin-B is 3- and 8-fold, respectively), when measured in a Ca2+ elevation assay and normalizing the data the orexin-A response [2], while a more recent study reported 420-fold selectivity for OX2 under similar conditions [3].
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. Asahi S, Egashira S, Matsuda M, Iwaasa H, Kanatani A, Ohkubo M, Ihara M, Morishima H. (2003)
Development of an orexin-2 receptor selective agonist, [Ala(11), D-Leu(15)]orexin-B.
Bioorg Med Chem Lett, 13 (1): 111-3. [PMID:12467628]
2. Putula J, Turunen PM, Jäntti MH, Ekholm ME, Kukkonen JP. (2011)
Agonist ligand discrimination by the two orexin receptors depends on the expression system.
Neurosci Lett, 494 (1): 57-60. [PMID:21362456]
3. Yamamoto H, Nagumo Y, Ishikawa Y, Irukayama-Tomobe Y, Namekawa Y, Nemoto T, Tanaka H, Takahashi G, Tokuda A, Saitoh T et al.. (2022)
OX2R-selective orexin agonism is sufficient to ameliorate cataplexy and sleep/wake fragmentation without inducing drug-seeking behavior in mouse model of narcolepsy.
PLoS One, 17 (7): e0271901. [PMID:35867683]