| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Opiranserin HCl targets glycine transporter type 2 (GlyT2), serotonin receptor 2A (5-HT2A), and the purinergic P2X3 receptor. GlyT2 is responsible for the reuptake of glycine in the spinal cord and brainstem, regulating inhibitory neurotransmission. 5-HT2A is a serotonin receptor involved in pain modulation and mood regulation. P2X3 is a purinergic receptor involved in pain signaling. The compound has IC50 values of 0.86 μM (GlyT2), 1.3 μM (5-HT2A), and 0.87 μM (P2X3).
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| ln Vitro |
In vitro, Opiranserin HCl inhibits GlyT2 with an IC50 of 0.86 μM and antagonizes 5-HT2A with an IC50 of 1.3 μM. It also shows antagonistic activity at the purinergic P2X3 receptor with an IC50 of 0.87 μM. The compound's dual mechanism of action contributes to its analgesic effects without opioid-related side effects. It has been studied for its potential applications in treating pain, depression, anxiety, and schizophrenia.
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| ln Vivo |
In vivo, Opiranserin HCl has been developed as an injectable analgesic for postoperative pain. As a non-opioid analgesic, it offers pain relief without the risk of opioid addiction or respiratory depression. Its dual antagonism of GlyT2 and 5-HT2A, along with P2X3 antagonism, provides a multimodal approach to pain management. However, specific in vivo efficacy data are not extensively detailed in the available literature.
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| Enzyme Assay |
In vitro enzyme/receptor binding assays for Opiranserin HCl typically involve radioligand binding assays for 5-HT2A and P2X3 receptors, and functional assays for GlyT2 inhibition. For GlyT2, cells expressing the transporter are incubated with 3H-glycine and various concentrations of the compound (typically 0.001-100 μM). Glycine uptake is measured by scintillation counting. For 5-HT2A and P2X3, membrane preparations are incubated with radiolabeled ligands and the compound, and bound radioactivity is measured. IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for Opiranserin HCl use cells expressing GlyT2, 5-HT2A, or P2X3 receptors. For GlyT2, cells are cultured in appropriate media and treated with various concentrations of the compound (0.001-100 μM), and glycine uptake is measured using 3H-glycine. For 5-HT2A, calcium mobilization is measured in cells stimulated with serotonin. For P2X3, ATP-induced calcium influx is measured. Receptor antagonism is assessed by inhibition of agonist-induced responses.
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| Animal Protocol |
In vivo animal studies with Opiranserin HCl would typically use rodent models of pain, such as the formalin test, hot plate test, or postoperative pain models. The compound would be administered intravenously or intraperitoneally at doses of 1-30 mg/kg. Pain behavior (licking, flinching, or withdrawal latency) is measured. The compound's analgesic efficacy is compared to opioid and NSAID controls. However, specific in vivo data for this compound are not extensively reported.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Opiranserin HCl: The compound is developed as an injectable formulation for postoperative pain. Specific PK parameters such as half-life, volume of distribution, and clearance are not extensively reported. The compound has a molecular weight of 430.97. As a small molecule, it is expected to have moderate protein binding and tissue distribution.
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| Toxicity/Toxicokinetics |
The toxicity profile of Opiranserin HCl is not extensively reported in the available literature. As a non-opioid analgesic, it is expected to have a favorable safety profile with reduced risk of addiction and respiratory depression compared to opioids. The compound is for research use only and not for human therapeutic use. Standard toxicity studies would include acute and subchronic toxicity in rodents.
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| References |
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| Additional Infomation |
Opiranserin HCl (CAS 1440796-75-7, VVZ-149) is a non-opioid, non-NSAID analgesic that is a dual antagonist of GlyT2 (IC50 = 0.86 μM) and 5-HT2A (IC50 = 1.3 μM), with additional P2X3 antagonism (IC50 = 0.87 μM). It has been developed as an injectable analgesic for postoperative pain. The compound has potential applications in pain, depression, anxiety, and schizophrenia research. It is available for research purposes only.
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| Molecular Formula |
C21H35CLN2O5
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|---|---|
| Molecular Weight |
430.97
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| Exact Mass |
430.223
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| CAS # |
1440796-75-7
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| Related CAS # |
Opiranserin;1441000-45-8
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| PubChem CID |
71566777
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
29
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| Complexity |
454
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(OCCCC)C(OC)=CC(C(NCC2(CCOCC2)N(C)C)=O)=C1.Cl
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| InChi Key |
GSCGQHXDHYVKOL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H34N2O5.ClH/c1-6-7-10-28-19-17(25-4)13-16(14-18(19)26-5)20(24)22-15-21(23(2)3)8-11-27-12-9-21;/h13-14H,6-12,15H2,1-5H3,(H,22,24);1H
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| Chemical Name |
4-butoxy-N-[[4-(dimethylamino)oxan-4-yl]methyl]-3,5-dimethoxybenzamide;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~116.02 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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