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G Protein-Coupled Receptor Ligands
- Protein Control Ligand
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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
Discontinued listing as Schedule II Controlled Substance
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Data sheet
| Molecular Formula | C22H30N2O2S |
| Molecular Weight | 386.55 |
| CAS Numbers | 1401031-39-7 |
| Storage Condition | 0°C (short term), -20°C (long term), desiccated |
| Solubility | DMSO and Alcohol |
| Purity | 98% by HPLC |
| 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 |
| InChl Key | YIIWXYLJZRISQP-ZMBIFBSDSA-N |
| InChl 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 |
| References | 1) 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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Novel MOR G protein-biased ligand