TRV130 hydrochloride (Oliceridine) is a functionally selective μ-opioid receptor agonist developed by Trevena Inc. TRV130 elicits robust G protein signaling, but with far less β-arrestin 2 recruitment and receptor internalization, it displays less adverse effects.
Anesth Analg. 2018 Jul 21.
Pharmacological Characters of Oliceridine, a μ-Opioid Receptor G-Protein[FIGURE DASH]Biased Ligand in Mice.
TRV130 hydrochloride purchased from AbMole
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Source | Anesthesia & Analgesia (2018 Jul). Figure 5. TRV-130 (Abmole Bioscience Inc, Houston, TX) |
| Method | CPP assay | |
| Cell Lines | mice | |
| Concentrations | 1.25 or 10 mg/kg | |
| Incubation Time | 7 d | |
| Results | Figure 5 shows that TLR4 mRNA expression was increased in the lumbar spinal cord tissue of fracture mice that received morphine at 3 weeks after injury(P < .05), while no such changes were observed in the fracture mice by the administration of oliceridine (P> .05). |
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Source | Anesthesia & Analgesia (2018 Jul). Figure 4. TRV-130 (Abmole Bioscience Inc, Houston, TX) |
| Method | CPP assay | |
| Cell Lines | mice | |
| Concentrations | 5 μL/injection | |
| Incubation Time | 7 d | |
| Results | The small amount of ethanol in the oliceridine vehicle (5 μL/injection) did not appear to affect nociceptive sensitivity as demonstrated in Figure 4. |
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Source | Anesthesia & Analgesia (2018 Jul). Figure 3. TRV-130 (Abmole Bioscience Inc, Houston, TX) |
| Method | CPP assay | |
| Cell Lines | mice | |
| Concentrations | 1.25 or 10 mg/kg | |
| Incubation Time | 3 d | |
| Results | However, a dose of oliceridine providing similar levels of analgesia, 1.25 mg/kg, did not cause statistically significant CPP (P > .05). |
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Source | Anesthesia & Analgesia (2018 Jul). Figure 2. TRV-130 (Abmole Bioscience Inc, Houston, TX) |
| Method | CPP assay | |
| Cell Lines | mice | |
| Concentrations | 1.25 or 10 mg/kg | |
| Incubation Time | 3 d | |
| Results | Figure 2 shows that both chronic oliceridine and morphine treatment reduced the mechanical paw withdraw thresholds in comparison with the baseline thresholds (P < .001). |
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Source | Anesthesia & Analgesia (2018 Jul). Figure 1. TRV-130 (Abmole Bioscience Inc, Houston, TX) |
| Method | chronic administration | |
| Cell Lines | mice | |
| Concentrations | 5 mg/kg twice per day on days 1-3 and on day 4, 10 mg/kg | |
| Incubation Time | 4 days | |
| Results | Figure 1A, B and the Table show that oliceridine dose–response curves were not significantly changed before and after chronic dosing (P > .05). |
 |
Source | J Psychopharmacol (2017). Figure 1. TRV130 |
| Method | injection | |
| Cell Lines | mice | |
| Concentrations | 100 nM | |
| Incubation Time | 24h | |
| Results | In the repeated-vehicle treatment group, vehicle administration on Day 4 did not produce antinociception, and mice displayed high fecal output, whereas 10 mg/kg (+)-TRV130 produced maximal antinociception in all mice and nearly maximal suppression of fecal output. In the 3-day (+)-TRV130 treatment group |
| Molecular Weight | 423.01 |
| Formula | C22H31ClN2O2S |
| CAS Number | 1401031-39-7 |
| Solubility (25°C) | DMSO ≥ 35 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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