Synonyms: Olinvyk® | TRV130 | TRV130A
oliceridine is an approved drug (FDA (2020))
Compound class:
Synthetic organic
Comment: Oliceridine (TRV130) is an opioid compound. It was developed to exhibit biased-signalling (specifically bias towards G protein signalling), with the aim of reducing the adverse effects associated with use of other opioid drugs [1-2].
Ligand Activity Visualisation ChartsThese 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. ✖ |
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References |
1. Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL et al.. (2013)
Structure-activity relationships and discovery of a G protein biased μ opioid receptor ligand, [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro-[4.5]decan-9-yl]ethyl})amine (TRV130), for the treatment of acute severe pain. J Med Chem, 56 (20): 8019-31. [PMID:24063433] |
2. DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C et al.. (2013)
A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine. J Pharmacol Exp Ther, 344 (3): 708-17. [PMID:23300227] |
3. Soergel DG, Ann Subach R, Sadler B, Connell J, Marion AS, Cowan CL, Violin JD, Lark MW. (2014)
First Clinical Experience With TRV130: Pharmacokinetics and Pharmacodynamics in Healthy Volunteers. J Clin Pharmacol, 54 (3): 351-7. [PMID:24122908] |