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G Protein-Coupled Receptor Ligands

TRV130 hydrochloride View larger

TRV130 hydrochloride

AOB37943

CAS: 1401031-39-7

 

Chemical Name: TRV130A; Oliceridine; [(3-methoxythiophen-2-yl)methyl]({2-[(9R)-9-(pyridin-2-yl)-6-oxaspiro[4.5]decan-9-yl]ethyl})amine hydrochloride

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Discontinued listing as Schedule II Controlled Substance

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Data sheet

Molecular FormulaC22H30N2O2S
Molecular Weight386.55
CAS Numbers1401031-39-7
Storage Condition0°C (short term), -20°C (long term), desiccated
SolubilityDMSO and Alcohol
Purity98% by HPLC
SynonymTRV130; 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
InChl KeyYIIWXYLJZRISQP-ZMBIFBSDSA-N
InChl CodeInChI=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 CodeCOC1=C(CNCC[C@@](C2)(C3=NC=CC=C3)CCOC42CCCC4)SC=C1.[H]Cl
References1) Soergel DG, Subach RA, Burnham N, Lark MW, James IE, Sadler BM, Skobieranda F, Violin JD, Webster LR. Biased agonism of the μ-opioid receptor by TRV130 increases analgesia and reduces on-target adverse effects versus morphine: A randomized, double-blind, placebo-controlled, crossover study in healthy volunteers. Pain. 2014 Sep;155(9):1829-35.

2) Violin JD, Crombie AL, Soergel DG, Lark MW. Biased ligands at G-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 May 28. Review. PubMed PMID: 24878326.

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