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Opiranserin

Catalog No. T16399 CAS 1441000-45-8

Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) (IC50s: 0.86 and 1.3 μM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μM).

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Opiranserin, CAS 1441000-45-8

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Purity: 98%

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Description	Opiranserin is a development as an injectable agent for the treatment of postoperative pain. Opiranserin is a non-opioid and non-NSAID analgesic candidate and is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A) (IC50s: 0.86 and 1.3 μM, respectively). Opiranserin displays antagonistic activity on rP2X3 (IC50=0.87 μM).
Targets&IC50	rP2X3:0.87 μM, 5-HT2A Receptor:1.3 μM, GlyT2:0.86 μM

Molecular Weight	394.51
Formula	C21H34N2O5
CAS No.	1441000-45-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

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):e011035. 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.

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Keywords

Opiranserin 1441000-45-8 G蛋白偶联受体离子通道神经科学 5-HT Receptor GlyT P2 Receptor P2X Receptor Glycine transporters postoperative VVZ-149 Serotonin Receptor 5-hydroxytryptamine Receptor VVZ 149 pain Inhibitor non-opioid P2XRs anti-inflammatory VVZ149 analgesic inhibit inhibitor

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