Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C22H30N2O2S.ClH |
| Molecular Weight | 423.012 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.COC1=C(CNCC[C@]2(CCOC3(CCCC3)C2)C4=NC=CC=C4)SC=C1
InChI
InChIKey=YIIWXYLJZRISQP-ZMBIFBSDSA-N
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
DescriptionCurator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23300227
Curator's Comment: Description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/23300227
Oliceridine (TRV-130) is a potent μ-opioid receptor agonist. In cell-based assays, TRV130 elicits robust G protein signaling, with potency and efficacy similar to morphine, but with far less β-arrestin recruitment and receptor internalization. In rodents, TRV130 is potently analgesic while causing less gastrointestinal dysfunction and respiratory suppression than morphine at equianalgesic doses. Oliceridine is being developed by Trevena for the first-line treatment of moderate-to-severe acute postoperative pain. Phase III development is underway for the treatment of postoperative pain in the US. Phase II development is underway for the treatment of acute pain in the US.
Originator
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| 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. | 2013 Oct 24 |
Patents
Sample Use Guides
Oliceridine dosed at 2mg or 3mg every 3 hours demonstrated a tolerability profile similar to morphine dosed at 4mg every 4 hours, in a randomised, double-blind, placebo-controlled, 48-hour phase IIa/b trial in patients with acute postoperative pain after bunionectomy
Route of Administration:
Intravenous
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
XNT4TDS88V
Created by
admin on Sat Dec 16 01:57:01 UTC 2023 , Edited by admin on Sat Dec 16 01:57:01 UTC 2023
|
PRIMARY | |||
|
68313941
Created by
admin on Sat Dec 16 01:57:01 UTC 2023 , Edited by admin on Sat Dec 16 01:57:01 UTC 2023
|
PRIMARY | |||
|
1401031-39-7
Created by
admin on Sat Dec 16 01:57:01 UTC 2023 , Edited by admin on Sat Dec 16 01:57:01 UTC 2023
|
PRIMARY |
SUBSTANCE RECORD
