Oliceridine HCl

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WARNING: This product is for research use only, not for human or veterinary use.

Description:Oliceridine, also known as TRV130,is a µ- opioid receptor agonist, that is currently 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. TRV130 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 less adverse effects than morphine. (http://en.wikipedia.org/wiki/TRV130).

Price and Availability

Oliceridine HCl, purity > 98%, is in stock. The same day shipping out after order is received.

Related CAS #:1401031-39-7 (HCl)1401028-24-7 (free base)

Synonym:TRV130; TRV 130; TRV130; Oliceridine; Oliceridine HCl; Oliceridine hydrochloride

IUPAC/Chemical Name:(R)-N-((3-methoxythiophen-2-yl)methyl)-2-(9-(pyridin-2-yl)-6-oxaspiro[4.5]decan-9-yl)ethanamine hydrochloride

InChi Key:YIIWXYLJZRISQP-ZMBIFBSDSA-N

InChi Code:InChI=1S/C22H30N2O2S.ClH/c1-25-18-7-15-27-19(18)16-23-13-10-21(20-6-2-5-12-24-20)11-14-26-22(17-21)8-3-4-9-22;/h2,5-7,12,15,23H,3-4,8-11,13-14,16-17H2,1H3;1H/t21-;/m1./s1

SMILES Code:COC1=C(CNCC[C@@](C2)(C3=NC=CC=C3)CCOC42CCCC4)SC=C1.[H]Cl

Technical Data

Additional Information

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. TRV130 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 less adverse effects than morphine. (https://en.wikipedia.org/wiki/TRV130).  

References

1: Soergel DG, Subach RA, Burnham N, Lark MW, JamesIE, Sadler BM, Skobieranda F, Violin JD, Webster LR. Biased agonism ofthe μ-opioid receptor by TRV130 increases analgesia and reduceson-target adverse effects versus morphine: A randomized, double-blind,placebo-controlled, crossover study in healthy volunteers. Pain. 2014Sep;155(9):1829-35. doi: 10.1016/j.pain.2014.06.011. Epub 2014 Jun 19.PubMed PMID: 24954166.

2: Violin JD, Crombie AL, Soergel DG, Lark MW. Biased ligands atG-protein-coupled receptors: promise and progress. Trends Pharmacol Sci.2014 Jul;35(7):308-16. doi: 10.1016/j.tips.2014.04.007. Epub 2014 May28. Review. PubMed PMID: 24878326.

3: Soergel DG, Subach RA, Sadler B, Connell J, Marion AS, Cowan CL,Violin JD, Lark MW. First clinical experience with TRV130:pharmacokinetics and pharmacodynamics in healthy volunteers. J ClinPharmacol. 2014 Mar;54(3):351-7. doi: 10.1002/jcph.207. Epub 2014 Jan28. PubMed PMID: 24122908.

4: Chen XT, Pitis P, Liu G, Yuan C, Gotchev D, Cowan CL, Rominger DH,Koblish M, Dewire SM, Crombie AL, Violin JD, Yamashita DS.Structure-activity relationships and discovery of a G protein biased μopioid 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. JMed Chem. 2013 Oct 24;56(20):8019-31. doi: 10.1021/jm4010829. Epub 2013Oct 14. PubMed PMID: 24063433.

5: 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. A Gprotein-biased ligand at the μ-opioid receptor is potently analgesicwith reduced gastrointestinal and respiratory dysfunction compared withmorphine. J Pharmacol Exp Ther. 2013 Mar;344(3):708-17. doi:10.1124/jpet.112.201616. Epub 2013 Jan 8. PubMed PMID: 23300227.

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