| Identification | Back Directory | [Name]
hydrochloride | [CAS]
1440796-75-7 | [Synonyms]
Opiranserin hydrochloride
4-butoxy-N-[[4-(dimethylamino)oxan-4-yl]methyl]-3,5-dimethoxybenzamide
hydrochloride
4-butoxy-N-[[4-(dimethylamino)oxan-4-yl]methyl]-3,5-dimethoxybenzamide
VVZ 149,analgesic,postoperative,VVZ-149,5-hydroxytryptamine Receptor,5-HT Receptor,anti-inflammatory,Opiranserin hydrochloride,Serotonin Receptor,Inhibitor,pain,GlyT,Opiranserin,non-opioid,inhibit,P2X Receptor,P2XRs,VVZ149,Glycine transporters | [Molecular Formula]
ClH | [MOL File]
1440796-75-7.mol | [Molecular Weight]
36.4609 |
| Hazard Information | Back Directory | [Uses]
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 IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain[1][2][3]. | [IC 50]
GlyT2: 0.86 μM (IC50); P2X3 Receptor; rP2X3: 0.87 μM (IC50); 5-HT2A Receptor: 1.3 μM (IC50) | [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. DOI:10.1002/jcph.973
[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):e011035. DOI:10.1136/bmjopen-2016-011035
[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. DOI:10.1016/j.drudis.2012.01.003 |
|
|