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Synonyms: APD-371 | APD371 | compound 6 [PMID: 29259753]
Compound class: Synthetic organic
Comment: Olorinab (APD371) is a cannabinoid CB2 receptor agonist that is being developed by Arena Pharmaceuticals as a potential treatment for chronic pain . In vitro, APD371 is as efficacious as the CB2 receptor full agonist CP55940 (as determined by measuring and comparing Emax values), and has limited tachyphylaxis liability (i.e. it does cause agonist-induced desensitization due to impeding the return of internalized agonist-activated receptors back to the plasma membrane) .
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.✖
1. Han S, Thoresen L, Jung JK, Zhu X, Thatte J, Solomon M, Gaidarov I, Unett DJ, Yoon WH, Barden J et al.. (2017)
Discovery of APD371: Identification of a Highly Potent and Selective CB2 Agonist for the Treatment of Chronic Pain.
ACS Med Chem Lett, 8 (12): 1309-1313. [PMID:29259753]