Oliceridine
From Wikipedia, the free encyclopedia
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| Systematic (IUPAC) name | |
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N-[(3-methoxythiophen-2-yl)methyl]-2-[(9R)-9-pyridin-2-yl-6-oxaspiro[4.5]decan-9-yl]ethanamine
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| Routes of administration |
IV |
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| Identifiers | |
| CAS Number | 1401028-24-7 |
| ATC code | none |
| PubChem | CID 66553195 |
| ChemSpider | 30841043 |
| UNII | MCN858TCP0 |
| ChEMBL | CHEMBL2443262 |
| Synonyms | TRV130 |
| Chemical data | |
| Formula | C22H30N2O2S |
| Molar mass | 386.55 g·mol−1 |
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Oliceridine (TRV130) is an opioid drug that is under evaluation in human clinical trials for the treatment of acute severe pain. It is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. Oliceridine elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin 2 recruitment and receptor internalization, it displays fewer adverse effects than morphine.[1][2][3][4]
References[edit]
- ^ Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH, Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS (October 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". Journal of Medicinal Chemistry. 56 (20): 8019–31. doi:10.1021/jm4010829. PMID 24063433. (subscription required (help)).
- ^ DeWire SM, Yamashita DS, Rominger DH, Liu G, Cowan CL, Graczyk TM, Chen XT, Pitis PM, Gotchev D, Yuan C, Koblish M, Lark MW, Violin JD (March 2013). "A G protein-biased ligand at the μ-opioid receptor is potently analgesic with reduced gastrointestinal and respiratory dysfunction compared with morphine". Journal of Pharmacology and Experimental Therapeutics. 344 (3): 708–17. doi:10.1124/jpet.112.201616. PMID 23300227.
- ^ Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan C, Violin JD, Lark MW (October 2013). "First clinical experience with TRV130: Pharmacokinetics and pharmacodynamics in healthy volunteers". The Journal of Clinical Pharmacology. 54 (3): 351–7. doi:10.1002/jcph.207. PMID 24122908. (subscription required (help)).
- ^ Staff (1 October 2015). "Acute Postoperative Pain". Genetic Engineering & Biotechnology News (Paper). 35 (17): 40.
External links[edit]
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