[CAS NO. 1440796-75-7] Opiranserin hydrochloride
PRODUCTS SPECIFICATIONS [1440796-75-7]
DESCRIPTION [1440796-75-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 430.97 |
| Molecular Formula | C21H35ClN2O5 |
| SMILES | O=C(C1=CC(OC)=C(OCCCC)C(OC)=C1)NCC2(CCOCC2)N(C)C.[H]Cl |
Summary
Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) , with IC 50 s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC 50 =0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain [1] [2] [3] .
IC50 & Target
|
GlyT2 0.86 μM (IC 50 ) |
rP2X3 0.87 μM (IC 50 ) |
5-HT 2A Receptor 1.3 μM (IC 50 ) |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02489526 | Vivozon, Inc. |
Post-Operative Pain
|
September 28, 2015 | Phase 2 |
| NCT02992041 | Vivozon, Inc. |
Post-Operative Pain
|
December 27, 2016 | Phase 2 |
| NCT03347266 | Vivozon, Inc. |
Post-Operative Pain
|
December 20, 2017 | Phase 2 |
| NCT03997812 | Vivozon, Inc. |
Pain, Postoperative
|
May 23, 2019 | Phase 2 |
| NCT02644421 | Brigham and Women´s Hospital |
Radiculopathy|Sciatica
|
November 2015 | Phase 1 |
| NCT02522598 | Vivozon, Inc. |
Post-Operative Pain
|
August 2015 | Phase 2 |
| NCT02844725 | Vivozon, Inc. |
Post-Operative Pain
|
June 2016 | Phase 2 |
| NCT03997838 | Vivozon, Inc. |
Pain, Postoperative
|
May 23, 2019 | Phase 3 |
| NCT01905410 | Vivozon, Inc. |
Healthy
|
July 2013 | Phase 1 |
| NCT02333318 | Vivozon, Inc. |
Healthy
|
July 2014 | Phase 1 |
| NCT04430088 | Vivozon, Inc. |
Pain, Postoperative
|
June 26, 2020 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 50 mg/mL ( 116.02 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3203 mL | 11.6017 mL | 23.2035 mL |
| 5 mM | 0.4641 mL | 2.3203 mL | 4.6407 mL |
| 10 mM | 0.2320 mL | 1.1602 mL | 2.3203 mL |
References
- [1] Oh J, et al. Safety, Tolerability, and Pharmacokinetic Characteristics of a Novel Nonopioid Analgesic, VVZ-149 Injections in Healthy Volunteers: A First-in-Class, First-in-Human Study. J Clin Pharmacol. 2018 Jan;58(1):64-73.
- [2] Nedeljkovic SS, et al. Randomised, double-blind, parallel group, placebo-controlled study to evaluate the analgesic efficacy and safety of VVZ-149 injections for postoperative pain following laparoscopic colorectal surgery. BMJ Open. 2017 Feb 17;7(2):e011
- [3] Pang MH, et al. A series of case studies: practical methodology for identifying antinociceptive multi-target drugs. Drug Discov Today. 2012 May;17(9-10):425-34.